Proteins > Peroxisome proliferator-activated receptor gamma
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Peroxisome proliferator-activated receptor gamma
A peroxisome proliferator-activated receptor gamma that is encoded in the genome of human. [PRO:DNx, UniProtKB:P37231]
Synonyms
PPAR-gamma;
Nuclear receptor subfamily 1 group C member 3
Research
Bioassay Publications (278)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 7 (2.52) | 18.2507 |
2000's | 111 (39.93) | 29.6817 |
2010's | 128 (46.04) | 24.3611 |
2020's | 32 (11.51) | 2.80 |
Compounds (110)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
gw 2433 | Homo sapiens (human) | EC50 | 2.5000 | 1 | 1 |
candesartan cilexetil | Homo sapiens (human) | EC50 | 4.2000 | 1 | 1 |
cannabinol | Homo sapiens (human) | EC50 | 25.0000 | 1 | 1 |
ciglitazone | Homo sapiens (human) | EC50 | 18.9044 | 2 | 2 |
clofibrate | Homo sapiens (human) | EC50 | 500.0000 | 2 | 2 |
clofibric acid | Homo sapiens (human) | EC50 | 221.3333 | 3 | 3 |
decanoic acid | Homo sapiens (human) | EC50 | 30.8000 | 2 | 2 |
fenofibrate | Homo sapiens (human) | EC50 | 157.7617 | 6 | 6 |
gemfibrozil | Homo sapiens (human) | EC50 | 121.3333 | 3 | 3 |
indomethacin | Homo sapiens (human) | EC50 | 50.0000 | 1 | 1 |
lg 100268 | Homo sapiens (human) | EC50 | 0.0725 | 3 | 3 |
pioglitazone | Homo sapiens (human) | EC50 | 0.8027 | 36 | 36 |
pioglitazone | Homo sapiens (human) | Kd | 0.8710 | 1 | 1 |
troglitazone | Homo sapiens (human) | EC50 | 1.1000 | 19 | 19 |
pirinixic acid | Homo sapiens (human) | EC50 | 29.2964 | 10 | 11 |
pirinixic acid | Homo sapiens (human) | Kd | 1.3186 | 2 | 2 |
ici 204,219 | Homo sapiens (human) | EC50 | 2.4400 | 1 | 1 |
3,3',5-triiodothyroacetic acid | Homo sapiens (human) | EC50 | 0.3700 | 1 | 1 |
3,3',5-triiodothyroacetic acid | Homo sapiens (human) | Kd | 0.2000 | 1 | 1 |
thyroxine | Homo sapiens (human) | EC50 | 12.0000 | 1 | 1 |
thyroxine | Homo sapiens (human) | Kd | 0.4000 | 1 | 1 |
triiodothyronine | Homo sapiens (human) | EC50 | 5.8000 | 1 | 1 |
triiodothyronine | Homo sapiens (human) | Kd | 0.7100 | 1 | 1 |
methyleugenol | Homo sapiens (human) | EC50 | 40.0000 | 1 | 1 |
cannabichromene | Homo sapiens (human) | EC50 | 25.0000 | 1 | 1 |
bezafibrate | Homo sapiens (human) | EC50 | 67.4250 | 12 | 12 |
pioglitazone hydrochloride | Homo sapiens (human) | EC50 | 4.0450 | 2 | 2 |
fenofibric acid | Homo sapiens (human) | EC50 | 171.8889 | 9 | 9 |
tetraiodothyroacetic acid | Homo sapiens (human) | EC50 | 0.1000 | 1 | 1 |
tetraiodothyroacetic acid | Homo sapiens (human) | Kd | 0.1100 | 1 | 1 |
telmisartan | Homo sapiens (human) | EC50 | 3.1277 | 13 | 13 |
rosiglitazone | Homo sapiens (human) | EC50 | 70.3876 | 147 | 147 |
rosiglitazone | Homo sapiens (human) | Kd | 1.2101 | 7 | 7 |
mk 767 | Homo sapiens (human) | EC50 | 0.7841 | 8 | 8 |
mk 767 | Homo sapiens (human) | Kd | 0.3280 | 2 | 2 |
jtt 501 | Homo sapiens (human) | EC50 | 0.0830 | 2 | 2 |
anacardic acid | Homo sapiens (human) | EC50 | 17.0000 | 1 | 1 |
farglitazar | Homo sapiens (human) | EC50 | 0.0020 | 16 | 16 |
l 158809 | Homo sapiens (human) | EC50 | 20.0000 | 1 | 1 |
muraglitazar | Homo sapiens (human) | EC50 | 0.2284 | 9 | 9 |
tesaglitazar | Homo sapiens (human) | EC50 | 2.3594 | 8 | 9 |
eicosapentaenoic acid | Homo sapiens (human) | Kd | 2.0000 | 1 | 1 |
mycophenolic acid | Homo sapiens (human) | Kd | 110.0000 | 1 | 1 |
gw 409544 | Homo sapiens (human) | EC50 | 0.0009 | 4 | 4 |
drf 2725 | Homo sapiens (human) | EC50 | 0.5800 | 6 | 6 |
epipinoresinol | Homo sapiens (human) | EC50 | 58.6000 | 1 | 1 |
cannabidiol | Homo sapiens (human) | EC50 | 25.0000 | 1 | 1 |
gw9662 | Homo sapiens (human) | EC50 | 0.0020 | 1 | 1 |
triiodothyronine, reverse | Homo sapiens (human) | EC50 | 3.8000 | 1 | 1 |
triiodothyronine, reverse | Homo sapiens (human) | Kd | 0.6300 | 1 | 1 |
sulindac | Homo sapiens (human) | EC50 | 22.6500 | 1 | 1 |
sulindac | Homo sapiens (human) | Kd | 100.0000 | 1 | 1 |
2-chloro-n(6)-(3-iodobenzyl)adenosine-5'-n-methyluronamide | Homo sapiens (human) | EC50 | 2.9400 | 1 | 1 |
rivoglitazone | Homo sapiens (human) | EC50 | 0.0430 | 1 | 1 |
gw 7647 | Homo sapiens (human) | EC50 | 1.1000 | 1 | 1 |
gw 7647 | Homo sapiens (human) | Kd | 0.1800 | 1 | 1 |
hydroxypioglitazone | Homo sapiens (human) | EC50 | 1.3600 | 3 | 3 |
hydroxypioglitazone | Homo sapiens (human) | Kd | 0.7080 | 1 | 1 |
alpha-linolenic acid | Homo sapiens (human) | Kd | 2.0000 | 1 | 1 |
clothiapine | Homo sapiens (human) | EC50 | 0.7300 | 1 | 1 |
psi-baptigenin | Homo sapiens (human) | EC50 | 26.9400 | 3 | 3 |
9-hydroxy-10,12-octadecadienoic acid | Homo sapiens (human) | Kd | 2.0000 | 1 | 1 |
15-deoxy-delta(12,14)-prostaglandin j2 | Homo sapiens (human) | Kd | 2.0000 | 1 | 1 |
cannabigerol | Homo sapiens (human) | EC50 | 15.7000 | 1 | 1 |
sulindac sulfide | Homo sapiens (human) | EC50 | 0.8000 | 2 | 2 |
psammaplin a | Homo sapiens (human) | EC50 | 5.7000 | 1 | 1 |
pregna-4,17-diene-3,16-dione | Homo sapiens (human) | EC50 | 100.0000 | 1 | 1 |
amorphastilbol | Homo sapiens (human) | EC50 | 5.0000 | 1 | 1 |
gw 1929 | Homo sapiens (human) | EC50 | 0.1025 | 15 | 18 |
l-165041 | Homo sapiens (human) | EC50 | 3.6620 | 2 | 2 |
gw 501516 | Homo sapiens (human) | EC50 | 5.1349 | 18 | 23 |
tzd 18 | Homo sapiens (human) | EC50 | 0.0127 | 3 | 3 |
efatutazone | Homo sapiens (human) | EC50 | 0.0005 | 2 | 2 |
lg 1506 | Homo sapiens (human) | EC50 | 0.0030 | 2 | 2 |
nrx 194204 | Homo sapiens (human) | EC50 | 0.0313 | 2 | 2 |
gft505 | Homo sapiens (human) | EC50 | 2.6780 | 4 | 4 |
3-(2,4-dichlorobenzyl)-2-methyl-n-(pentylsulfonyl)-3 h-benzimidazole-5-carboxamide | Homo sapiens (human) | EC50 | 0.3315 | 2 | 2 |
gw 9578 | Homo sapiens (human) | EC50 | 0.8410 | 8 | 8 |
gw 7845 | Homo sapiens (human) | EC50 | 0.0007 | 5 | 5 |
naveglitazar | Homo sapiens (human) | EC50 | 0.3805 | 2 | 2 |
ly 465608 | Homo sapiens (human) | EC50 | 0.8807 | 3 | 3 |
l 796449 | Homo sapiens (human) | EC50 | 0.0071 | 2 | 2 |
gw0742 | Homo sapiens (human) | EC50 | 5.7650 | 2 | 2 |
3-chloro-4-(3-(7-propyl-3-trifluoromethyl-6-benzisoxazolyl)propylthio)phenylacetic acid | Homo sapiens (human) | EC50 | 0.0230 | 1 | 1 |
ns-220 | Homo sapiens (human) | EC50 | 7.8167 | 3 | 3 |
bm 131246 | Homo sapiens (human) | EC50 | 0.0056 | 2 | 2 |
gw 590735 | Homo sapiens (human) | EC50 | 7.7805 | 6 | 8 |
int 131 | Homo sapiens (human) | EC50 | 0.1766 | 5 | 5 |
aleglitazar | Homo sapiens (human) | EC50 | 0.0210 | 1 | 1 |
msdc-0160 | Homo sapiens (human) | EC50 | 0.6570 | 1 | 1 |
mbx-8025 | Homo sapiens (human) | EC50 | 3.0000 | 2 | 2 |
cannabidiol hydroxyquinone | Homo sapiens (human) | EC50 | 10.5000 | 1 | 1 |
lt175 | Homo sapiens (human) | EC50 | 0.4642 | 8 | 10 |
lj 529 | Homo sapiens (human) | EC50 | 4.6400 | 1 | 1 |
arhalofenate | Homo sapiens (human) | EC50 | 6.6217 | 3 | 3 |
odoratin | Homo sapiens (human) | EC50 | 3.1000 | 1 | 1 |
bms 687453 | Homo sapiens (human) | EC50 | 3.6532 | 4 | 4 |
amorfrutin a | Homo sapiens (human) | EC50 | 0.4580 | 2 | 2 |
amorfrutin a | Homo sapiens (human) | Kd | 0.2360 | 1 | 1 |
amorfrutin b | Homo sapiens (human) | EC50 | 0.0615 | 2 | 2 |
amorfrutin b | Homo sapiens (human) | Kd | 0.0190 | 1 | 1 |
ys 121 | Homo sapiens (human) | EC50 | 3.6000 | 2 | 2 |
[5-fluoro-1-(4-isopropylbenzylidene)-2-methylinden-3-yl]acetic acid | Homo sapiens (human) | EC50 | 50.0000 | 1 | 1 |
[5-fluoro-1-(4-isopropylbenzylidene)-2-methylinden-3-yl]acetic acid | Homo sapiens (human) | Kd | 100.0000 | 1 | 1 |
sr1664 | Homo sapiens (human) | EC50 | 4.2880 | 1 | 1 |
Drugs with Other Measurements
PPARγ-sparing thiazolidinediones as insulin sensitizers. Design, synthesis and selection of compounds for clinical development.Bioorganic & medicinal chemistry, , 12-01, Volume: 26, Issue:22, 2018
Two new furanoditerpenes from Saururus chinenesis and their effects on the activation of peroxisome proliferator-activated receptor gamma.Journal of natural products, , Volume: 65, Issue:4, 2002
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents.Journal of medicinal chemistry, , Dec-03, Volume: 41, Issue:25, 1998
Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 2004
The PPARs: from orphan receptors to drug discovery.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonists. 1. Discovery of a novel series of potent HDLc raising agents.Journal of medicinal chemistry, , Feb-22, Volume: 50, Issue:4, 2007
Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARalpha and PPARgamma agonist activity.Journal of medicinal chemistry, , Aug-25, Volume: 48, Issue:17, 2005
A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARalpha agonist with potent lipid-lowering activity.Journal of medicinal chemistry, , Sep-23, Volume: 42, Issue:19, 1999
Phenolic Lipids Derived from Cashew Nut Shell Liquid to Treat Metabolic Diseases.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
[no title available]Journal of medicinal chemistry, , 01-28, Volume: 64, Issue:2, 2021
The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.Journal of medicinal chemistry, , Jul-23, Volume: 52, Issue:14, 2009
Omega-(2-Naphthyloxy) amino alkanes as a novel class of anti-hyperglycemic and lipid lowering agents.Bioorganic & medicinal chemistry, , Mar-01, Volume: 16, Issue:5, 2008
Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 2004
Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template.Bioorganic & medicinal chemistry letters, , Jan-20, Volume: 13, Issue:2, 2003
The PPARs: from orphan receptors to drug discovery.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
Synthesis and Evaluation of PPARδ Agonists That Promote Osteogenesis in a Human Mesenchymal Stem Cell Culture and in a Mouse Model of Human Osteoporosis.Journal of medicinal chemistry, , 05-27, Volume: 64, Issue:10, 2021
Design, synthesis, and biological evaluation of novel constrained meta-substituted phenyl propanoic acids as peroxisome proliferator-activated receptor alpha and gamma dual agonists.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARalpha/gamma dual agonists.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 17, Issue:13, 2007
Design and synthesis of novel RXR-selective modulators with improved pharmacological profile.Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 13, Issue:22, 2003
Novel (2E,4E,6Z)-7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta-2,4,6-trienoic acid retinoid X receptor modulators are active in models of type 2 diabetes.Journal of medicinal chemistry, , Jun-19, Volume: 46, Issue:13, 2003
Discovery of Pan-peroxisome Proliferator-Activated Receptor Modulators from an Endolichenic Fungus, Journal of natural products, , 12-23, Volume: 85, Issue:12, 2022
Identification and development of non-cytotoxic cell death modulators: Impact of sartans and derivatives on PPARγ activation and on growth of imatinib-resistant chronic myelogenous leukemia cells.European journal of medicinal chemistry, , Jun-01, Volume: 195, 2020
[no title available]Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Overcoming imatinib resistance in chronic myelogenous leukemia cells using non-cytotoxic cell death modulators.European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Adiponectin-Secretion-Promoting Phenylethylchromones from the Agarwood of Aquilaria malaccensis.Journal of natural products, , 02-22, Volume: 82, Issue:2, 2019
2-Phenyl-8-(1-phenylallyl)-chromenone compounds have a pan-PPAR modulator pharmacophore.Bioorganic & medicinal chemistry, , 07-01, Volume: 27, Issue:13, 2019
Structural Basis of Altered Potency and Efficacy Displayed by a Major in Vivo Metabolite of the Antidiabetic PPARγ Drug Pioglitazone.Journal of medicinal chemistry, , 02-28, Volume: 62, Issue:4, 2019
[no title available]Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
PPARγ-sparing thiazolidinediones as insulin sensitizers. Design, synthesis and selection of compounds for clinical development.Bioorganic & medicinal chemistry, , 12-01, Volume: 26, Issue:22, 2018
Stereoselective Synthesis of the Isomers of Notoincisol A: Assigment of the Absolute Configuration of this Natural Product and Biological Evaluation.Journal of natural products, , 11-26, Volume: 81, Issue:11, 2018
Design, synthesis, and evaluation of novel l-phenylglycine derivatives as potential PPARγ lead compounds.Bioorganic & medicinal chemistry, , 08-07, Volume: 26, Issue:14, 2018
Structure-activity relationships of rosiglitazone for peroxisome proliferator-activated receptor gamma transrepression.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 27, Issue:12, 2017
Importance of 5/6-aryl substitution on the pharmacological profile of 4'-((2-propyl-1H-benzo[d]imidazol-1-yl)methyl)-[1,1'-biphenyl]-2-carboxylic acid derived PPARγ agonists.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
Evaluation of selected 3D virtual screening tools for the prospective identification of peroxisome proliferator-activated receptor (PPAR) γ partial agonists.European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
New telmisartan-derived PPARγ agonists: Impact of the 3D-binding mode on the pharmacological profile.European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
N-Benzylbenzamides: A Novel Merged Scaffold for Orally Available Dual Soluble Epoxide Hydrolase/Peroxisome Proliferator-Activated Receptor γ Modulators.Journal of medicinal chemistry, , Jan-14, Volume: 59, Issue:1, 2016
Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 25, Issue:15, 2015
Polyyne hybrid compounds from Notopterygium incisum with peroxisome proliferator-activated receptor gamma agonistic effects.Journal of natural products, , Nov-26, Volume: 77, Issue:11, 2014
Design, synthesis, and evaluation of imidazo[4,5-c]pyridin-4-one derivatives with dual activity at angiotensin II type 1 receptor and peroxisome proliferator-activated receptor-γ.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 23, Issue:3, 2013
Sesquiterpene lactones from Tithonia diversifolia act as peroxisome proliferator-activated receptor agonists.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 22, Issue:8, 2012
Synthesis, biological evaluation and molecular investigation of fluorinated peroxisome proliferator-activated receptors α/γ dual agonists.Bioorganic & medicinal chemistry, , Mar-15, Volume: 20, Issue:6, 2012
Design and synthesis of dual modulators of soluble epoxide hydrolase and peroxisome proliferator-activated receptors.Journal of medicinal chemistry, , Dec-13, Volume: 55, Issue:23, 2012
Synthesis and structure-activity relationships of fibrate-based analogues inside PPARs.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 22, Issue:24, 2012
Synthesis and pharmacological evaluation of novel benzoylazole-based PPAR α/γ activators.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 21, Issue:7, 2011
Discovery of a series of imidazo[4,5-b]pyridines with dual activity at angiotensin II type 1 receptor and peroxisome proliferator-activated receptor-γ.Journal of medicinal chemistry, , Jun-23, Volume: 54, Issue:12, 2011
Development of a new class of benzoylpyrrole-based PPARα/γ activators.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
SAR studies of acidic dual γ-secretase/PPARγ modulators.Bioorganic & medicinal chemistry, , Sep-15, Volume: 19, Issue:18, 2011
Characterization of new PPARgamma agonists: benzimidazole derivatives-importance of positions 5 and 6, and computational studies on the binding mode.Bioorganic & medicinal chemistry, , Aug-15, Volume: 18, Issue:16, 2010
Rational design of a pirinixic acid derivative that acts as subtype-selective PPARgamma modulator.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
1,3-Diphenyl-1H-pyrazole derivatives as a new series of potent PPARγ partial agonists.Bioorganic & medicinal chemistry, , Dec-01, Volume: 18, Issue:23, 2010
Discovery of a novel selective PPARgamma modulator from (-)-Cercosporamide derivatives.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 20, Issue:7, 2010
Design and synthesis of 6-methyl-2-oxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylic acid derivatives as PPARgamma activators.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 17, Issue:16, 2007
Design and synthesis of the first generation of dithiolane thiazolidinedione- and phenylacetic acid-based PPARgamma agonists.Journal of medicinal chemistry, , Jul-13, Volume: 49, Issue:14, 2006
Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.Journal of medicinal chemistry, , Nov-06, Volume: 46, Issue:23, 2003
Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.Journal of medicinal chemistry, , Feb-14, Volume: 45, Issue:4, 2002
Synthesis and biological activity of L-tyrosine-based PPARgamma agonists with reduced molecular weight.Bioorganic & medicinal chemistry letters, , Dec-17, Volume: 11, Issue:24, 2001
The PPARs: from orphan receptors to drug discovery.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
Synthesis and biological activity of a novel series of indole-derived PPARgamma agonists.Bioorganic & medicinal chemistry letters, , Dec-06, Volume: 9, Issue:23, 1999
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents.Journal of medicinal chemistry, , Dec-03, Volume: 41, Issue:25, 1998
Galangin 3-benzyl-5-methylether derivatives function as an adiponectin synthesis-promoting peroxisome proliferator-activated receptor γ partial agonist.Bioorganic & medicinal chemistry, , 01-15, Volume: 54, 2022
Discovery of (Journal of medicinal chemistry, , 07-28, Volume: 65, Issue:14, 2022
[no title available]Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Selenium bioisosteric replacement of adenosine derivatives promoting adiponectin secretion increases the binding affinity to peroxisome proliferator-activated receptor δ.Bioorganic & medicinal chemistry, , 01-01, Volume: 28, Issue:1, 2020
Discovery of a Novel Selective Dual Peroxisome Proliferator-Activated Receptor α/δ Agonist for the Treatment of Primary Biliary Cirrhosis.ACS medicinal chemistry letters, , Jul-11, Volume: 10, Issue:7, 2019
Kojyl cinnamate esters are peroxisome proliferator-activated receptor α/γ dual agonists.Bioorganic & medicinal chemistry, , 11-15, Volume: 26, Issue:21, 2018
PPARγ-sparing thiazolidinediones as insulin sensitizers. Design, synthesis and selection of compounds for clinical development.Bioorganic & medicinal chemistry, , 12-01, Volume: 26, Issue:22, 2018
2-Formyl-komarovicine promotes adiponectin production in human mesenchymal stem cells through PPARγ partial agonism.Bioorganic & medicinal chemistry, , 03-01, Volume: 26, Issue:5, 2018
Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 25, Issue:15, 2015
Adipogenetic effects of retrofractamide A derivatives in 3T3-L1 cells.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
Sesquiterpene lactones from Tithonia diversifolia act as peroxisome proliferator-activated receptor agonists.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 22, Issue:8, 2012
Diarylheptanoid glycosides from Tacca plantaginea and their effects on NF-κB activation and PPAR transcriptional activity.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 22, Issue:21, 2012
Polyhydroxylated macrolides from Seimatosporium discosioides and their effects on the activation of peroxisome proliferator-activated receptor gamma.Journal of natural products, , Apr-27, Volume: 75, Issue:4, 2012
Anti-inflammatory and PPAR transactivational effects of secondary metabolites from the roots of Asarum sieboldii.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 22, Issue:7, 2012
Total synthesis and dual PPARα/γ agonist effects of amorphastilbol and its synthetic derivatives.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 22, Issue:12, 2012
Acetylenic acid analogues from the edible mushroom Chanterelle (Cantharellus cibarius) and their effects on the gene expression of peroxisome proliferator-activated receptor-gamma target genes.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 22, Issue:6, 2012
Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro.Journal of natural products, , Aug-26, Volume: 74, Issue:8, 2011
Effects of amide constituents from pepper on adipogenesis in 3T3-L1 cells.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 18, Issue:11, 2008
Tetrahydroisoquinoline PPARgamma agonists: design of novel, highly selective non-TZD antihyperglycemic agents.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 16, Issue:24, 2006
Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.Journal of medicinal chemistry, , Feb-14, Volume: 45, Issue:4, 2002
Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists.Journal of medicinal chemistry, , Jun-21, Volume: 44, Issue:13, 2001
The PPARs: from orphan receptors to drug discovery.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
Synthesis and biological activity of a novel series of indole-derived PPARgamma agonists.Bioorganic & medicinal chemistry letters, , Dec-06, Volume: 9, Issue:23, 1999
Novel antidiabetic and hypolipidemic agents. 3. Benzofuran-containing thiazolidinediones.Journal of medicinal chemistry, , Jun-03, Volume: 42, Issue:11, 1999
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents.Journal of medicinal chemistry, , Dec-03, Volume: 41, Issue:25, 1998
Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation.Journal of medicinal chemistry, , 02-28, Volume: 62, Issue:4, 2019
New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.European journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
Identification of pirinixic acid derivatives bearing a 2-aminothiazole moiety combines dual PPARα/γ activation and dual 5-LO/mPGES-1 inhibition.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 24, Issue:16, 2014
Molecular determinants for improved activity at PPARα: structure-activity relationship of pirinixic acid derivatives, docking study and site-directed mutagenesis of PPARα.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 24, Issue:16, 2014
Rational design of a pirinixic acid derivative that acts as subtype-selective PPARgamma modulator.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
Synthesis, biological evaluation, and molecular modeling investigation of chiral 2-(4-chloro-phenoxy)-3-phenyl-propanoic acid derivatives with PPARalpha and PPARgamma agonist activity.Bioorganic & medicinal chemistry, , Nov-01, Volume: 16, Issue:21, 2008
Design of potent PPARalpha agonists.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 17, Issue:11, 2007
Synthesis of new carbo- and heterocyclic analogues of 8-HETE and evaluation of their activity towards the PPARs.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 15, Issue:20, 2005
Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.Journal of medicinal chemistry, , Nov-06, Volume: 46, Issue:23, 2003
Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.Journal of medicinal chemistry, , Feb-14, Volume: 45, Issue:4, 2002
The PPARs: from orphan receptors to drug discovery.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
The discovery of novel isoflavone pan peroxisome proliferator-activated receptor agonists.Bioorganic & medicinal chemistry, , Feb-01, Volume: 21, Issue:3, 2013
Diarylheptanoid glycosides from Tacca plantaginea and their effects on NF-κB activation and PPAR transcriptional activity.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 22, Issue:21, 2012
Effect of structurally constrained oxime-ether linker on PPAR subtype selectivity: Discovery of a novel and potent series of PPAR-pan agonists.Bioorganic & medicinal chemistry, , Jan-15, Volume: 19, Issue:2, 2011
Structure-activity studies on 1,3-dioxane-2-carboxylic acid derivatives, a novel class of subtype-selective peroxisome proliferator-activated receptor alpha (PPARalpha) agonists.Bioorganic & medicinal chemistry, , Jan-15, Volume: 16, Issue:2, 2008
Discovery of a novel class of 1,3-dioxane-2-carboxylic acid derivatives as subtype-selective peroxisome proliferator-activated receptor alpha (PPARalpha) agonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 18, Issue:6, 2008
Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonists. 1. Discovery of a novel series of potent HDLc raising agents.Journal of medicinal chemistry, , Feb-22, Volume: 50, Issue:4, 2007
Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 2004
Design, synthesis, and evaluation of substituted phenylpropanoic acid derivatives as human peroxisome proliferator activated receptor activators. Discovery of potent and human peroxisome proliferator activated receptor alpha subtype-selective activators.Journal of medicinal chemistry, , Aug-14, Volume: 46, Issue:17, 2003
Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.Journal of medicinal chemistry, , Feb-14, Volume: 45, Issue:4, 2002
Design, synthesis and evaluation of substituted phenylpropanoic acid derivatives as peroxisome proliferator-activated receptor (PPAR) activators: novel human PPARalpha-selective activators.Bioorganic & medicinal chemistry letters, , Jan-07, Volume: 12, Issue:1, 2002
The PPARs: from orphan receptors to drug discovery.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARalpha agonist with potent lipid-lowering activity.Journal of medicinal chemistry, , Sep-23, Volume: 42, Issue:19, 1999
Novel 5-substituted 2,4-thiazolidinedione and 2,4-oxazolidinedione derivatives as insulin sensitizers with antidiabetic activities.Journal of medicinal chemistry, , Mar-28, Volume: 45, Issue:7, 2002
Novel oximes having 5-benzyl-2,4-thiazolidinedione as antihyperglycemic agents: synthesis and structure-activity relationship.Bioorganic & medicinal chemistry letters, , Feb-21, Volume: 10, Issue:4, 2000
The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
New 2-aryloxy-3-phenyl-propanoic acids as peroxisome proliferator-activated receptors alpha/gamma dual agonists with improved potency and reduced adverse effects on skeletal muscle function.Journal of medicinal chemistry, , Oct-22, Volume: 52, Issue:20, 2009
Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.Bioorganic & medicinal chemistry letters, , May-01, Volume: 19, Issue:9, 2009
Structure-activity studies on 1,3-dioxane-2-carboxylic acid derivatives, a novel class of subtype-selective peroxisome proliferator-activated receptor alpha (PPARalpha) agonists.Bioorganic & medicinal chemistry, , Jan-15, Volume: 16, Issue:2, 2008
Discovery of a novel class of 1,3-dioxane-2-carboxylic acid derivatives as subtype-selective peroxisome proliferator-activated receptor alpha (PPARalpha) agonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 18, Issue:6, 2008
Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonists. 1. Discovery of a novel series of potent HDLc raising agents.Journal of medicinal chemistry, , Feb-22, Volume: 50, Issue:4, 2007
Synthesis and evaluation of aminomethyl dihydrocinnamates as a new class of PPAR ligands.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 16, Issue:24, 2006
Tetrahydroisoquinoline PPARgamma agonists: design of novel, highly selective non-TZD antihyperglycemic agents.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 16, Issue:24, 2006
2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents.Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 15, Issue:1, 2005
Discovery of a novel series of peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes and dyslipidemia.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose andJournal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARalpha agonist with potent lipid-lowering activity.Journal of medicinal chemistry, , Sep-23, Volume: 42, Issue:19, 1999
Identification and development of non-cytotoxic cell death modulators: Impact of sartans and derivatives on PPARγ activation and on growth of imatinib-resistant chronic myelogenous leukemia cells.European journal of medicinal chemistry, , Jun-01, Volume: 195, 2020
Overcoming imatinib resistance in chronic myelogenous leukemia cells using non-cytotoxic cell death modulators.European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
Multitarget PPARγ agonists as innovative modulators of the metabolic syndrome.European journal of medicinal chemistry, , Jul-01, Volume: 173, 2019
Importance of 5/6-aryl substitution on the pharmacological profile of 4'-((2-propyl-1H-benzo[d]imidazol-1-yl)methyl)-[1,1'-biphenyl]-2-carboxylic acid derived PPARγ agonists.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
Evaluation of selected 3D virtual screening tools for the prospective identification of peroxisome proliferator-activated receptor (PPAR) γ partial agonists.European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
New telmisartan-derived PPARγ agonists: Impact of the 3D-binding mode on the pharmacological profile.European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
Peroxisome Proliferator-Activated Receptor γ (PPARγ) and Ligand Choreography: Newcomers Take the Stage.Journal of medicinal chemistry, , Jul-23, Volume: 58, Issue:14, 2015
Discovery of novel indazole derivatives as dual angiotensin II antagonists and partial PPARγ agonists.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 24, Issue:4, 2014
Design, synthesis, and evaluation of imidazo[4,5-c]pyridin-4-one derivatives with dual activity at angiotensin II type 1 receptor and peroxisome proliferator-activated receptor-γ.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 23, Issue:3, 2013
Discovery of a series of imidazo[4,5-b]pyridines with dual activity at angiotensin II type 1 receptor and peroxisome proliferator-activated receptor-γ.Journal of medicinal chemistry, , Jun-23, Volume: 54, Issue:12, 2011
Characterization of new PPARgamma agonists: benzimidazole derivatives-importance of positions 5 and 6, and computational studies on the binding mode.Bioorganic & medicinal chemistry, , Aug-15, Volume: 18, Issue:16, 2010
Synthesis and biological activities of novel indole derivatives as potent and selective PPARgamma modulators.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 20, Issue:4, 2010
Design, synthesis, and biological evaluation of novel dual FFA1 and PPARδ agonists possessing phenoxyacetic acid scaffold.Bioorganic & medicinal chemistry, , 02-15, Volume: 56, 2022
Discovery of new and highly effective quadruple FFA1 and PPARα/γ/δ agonists as potential anti-fatty liver agents.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
A chemoinformatics search for peroxisome proliferator-activated receptors ligands revealed a new pan-agonist able to reduce lipid accumulation and improve insulin sensitivity.European journal of medicinal chemistry, , May-05, Volume: 235, 2022
Phenolic Lipids Derived from Cashew Nut Shell Liquid to Treat Metabolic Diseases.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Indazole MRL-871 interacts with PPARγ via a binding mode that induces partial agonism.Bioorganic & medicinal chemistry, , 08-15, Volume: 68, 2022
Discovery by Virtual Screening of an Inhibitor of CDK5-Mediated PPARγ Phosphorylation.ACS medicinal chemistry letters, , Apr-14, Volume: 13, Issue:4, 2022
[no title available]Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Structure-Based Design of Dual Partial Peroxisome Proliferator-Activated Receptor γ Agonists/Soluble Epoxide Hydrolase Inhibitors.Journal of medicinal chemistry, , 12-09, Volume: 64, Issue:23, 2021
Synthesis and Evaluation of PPARδ Agonists That Promote Osteogenesis in a Human Mesenchymal Stem Cell Culture and in a Mouse Model of Human Osteoporosis.Journal of medicinal chemistry, , 05-27, Volume: 64, Issue:10, 2021
[no title available]Journal of medicinal chemistry, , 01-28, Volume: 64, Issue:2, 2021
Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome.European journal of medicinal chemistry, , Dec-05, Volume: 225, 2021
Design, synthesis, and biological evaluation of a novel dual peroxisome proliferator-activated receptor alpha/delta agonist for the treatment of diabetic kidney disease through anti-inflammatory mechanisms.European journal of medicinal chemistry, , Jun-05, Volume: 218, 2021
Combined Cardioprotective and Adipocyte Browning Effects Promoted by the Eutomer of Dual sEH/PPARγ Modulator.Journal of medicinal chemistry, , 03-11, Volume: 64, Issue:5, 2021
Evolution of a 4-Benzyloxy-benzylamino Chemotype to Provide Efficacious, Potent, and Isoform Selective PPARα Agonists as Leads for Retinal Disorders.Journal of medicinal chemistry, , 03-26, Volume: 63, Issue:6, 2020
A Selective Modulator of Peroxisome Proliferator-Activated Receptor γ with an Unprecedented Binding Mode.Journal of medicinal chemistry, , 05-14, Volume: 63, Issue:9, 2020
[no title available]Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation.Journal of medicinal chemistry, , 02-28, Volume: 62, Issue:4, 2019
Novel Phenyldiazenyl Fibrate Analogues as PPAR α/γ/δ Pan-Agonists for the Amelioration of Metabolic Syndrome.ACS medicinal chemistry letters, , Apr-11, Volume: 10, Issue:4, 2019
Novel berberine-based derivatives with potent hypoglycemic activity.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 29, Issue:23, 2019
[no title available]Journal of natural products, , 07-26, Volume: 82, Issue:7, 2019
Design, synthesis, and evaluation of potent novel peroxisome proliferator-activated receptor γ indole partial agonists.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 29, Issue:22, 2019
Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.Bioorganic & medicinal chemistry, , 10-01, Volume: 26, Issue:18, 2018
Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.European journal of medicinal chemistry, , Jul-15, Volume: 155, 2018
PPARγ-sparing thiazolidinediones as insulin sensitizers. Design, synthesis and selection of compounds for clinical development.Bioorganic & medicinal chemistry, , 12-01, Volume: 26, Issue:22, 2018
Structure-guided evolution of a 2-phenyl-4-carboxyquinoline chemotype into PPARα selective agonists: New leads for oculovascular conditions.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 28, Issue:16, 2018
Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.Bioorganic & medicinal chemistry, , 10-01, Volume: 26, Issue:18, 2018
Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.European journal of medicinal chemistry, , Nov-05, Volume: 159, 2018
Identification of the First PPARα/γ Dual Agonist Able To Bind to Canonical and Alternative Sites of PPARγ and To Inhibit Its Cdk5-Mediated Phosphorylation.Journal of medicinal chemistry, , 09-27, Volume: 61, Issue:18, 2018
Synthesis, biological evaluation, and molecular docking investigation of benzhydrol- and indole-based dual PPAR-γ/FFAR1 agonists.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 28, Issue:9, 2018
Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.Journal of medicinal chemistry, , 03-22, Volume: 61, Issue:6, 2018
Anti-diabetic activity of fused PPARγ-SIRT1 ligands with limited body-weight gain by mimicking calorie restriction and decreasing SGK1 expression.European journal of medicinal chemistry, , Sep-08, Volume: 137, 2017
New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.European journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
Design, synthesis, molecular modeling and anti-hyperglycemic evaluation of novel quinoxaline derivatives as potential PPARγ and SUR agonists.Bioorganic & medicinal chemistry, , 02-15, Volume: 25, Issue:4, 2017
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.European journal of medicinal chemistry, , Sep-29, Volume: 138, 2017
Design, synthesis, molecular modeling and anti-hyperglycemic evaluation of quinazolin-4(3H)-one derivatives as potential PPARγ and SUR agonists.Bioorganic & medicinal chemistry, , 09-01, Volume: 25, Issue:17, 2017
Switching subtype-selectivity: Fragment replacement strategy affords novel class of peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists.Bioorganic & medicinal chemistry letters, , 07-15, Volume: 27, Issue:14, 2017
Structure-activity relationships of rosiglitazone for peroxisome proliferator-activated receptor gamma transrepression.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 27, Issue:12, 2017
A novel structural class of coumarin-chalcone fibrates as PPARα/γ agonists with potent antioxidant activities: Design, synthesis, biological evaluation and molecular docking studies.European journal of medicinal chemistry, , Sep-29, Volume: 138, 2017
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Discovery of N-(1-(3-(4-phenoxyphenyl)-1,2,4-oxadiazol-5-yl)ethyl)acetamides as novel acetyl-CoA carboxylase 2 (ACC2) inhibitors with peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonistic activity.Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Design and synthesis of novel Y-shaped barbituric acid derivatives as PPARγ activators.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Structure-activity relationship studies of non-carboxylic acid peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists.Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175.European journal of medicinal chemistry, , Jan-27, Volume: 90, 2015
Structural development studies of PPARs ligands based on tyrosine scaffold.European journal of medicinal chemistry, , Jan-07, Volume: 89, 2015
Novel Oxazolidinone-Based Peroxisome Proliferator Activated Receptor Agonists: Molecular Modeling, Synthesis, and Biological Evaluation.Journal of medicinal chemistry, , Aug-27, Volume: 58, Issue:16, 2015
Separation and peroxisome proliferator-activated receptor-γ agonist activity evaluation of synthetic racemic bavachinin enantiomers.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 25, Issue:12, 2015
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 24, Issue:22, 2014
Sterol fatty acid esters from the mushroom Hericium erinaceum and their PPAR transactivational effects.Journal of natural products, , Dec-26, Volume: 77, Issue:12, 2014
Structure-based identification of novel PPAR gamma ligands.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 23, Issue:21, 2013
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Molecular determinants for nuclear receptors selectivity: chemometric analysis, dockings and site-directed mutagenesis of dual peroxisome proliferator-activated receptors α/γ agonists.European journal of medicinal chemistry, , Volume: 63, 2013
Discovery of INT131: a selective PPARγ modulator that enhances insulin sensitivity.Bioorganic & medicinal chemistry, , Feb-15, Volume: 21, Issue:4, 2013
New 2-(aryloxy)-3-phenylpropanoic acids as peroxisome proliferator-activated receptor α/γ dual agonists able to upregulate mitochondrial carnitine shuttle system gene expression.Journal of medicinal chemistry, , Jan-10, Volume: 56, Issue:1, 2013
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
The discovery of novel isoflavone pan peroxisome proliferator-activated receptor agonists.Bioorganic & medicinal chemistry, , Feb-01, Volume: 21, Issue:3, 2013
Structural characterization of amorfrutins bound to the peroxisome proliferator-activated receptor γ.Journal of medicinal chemistry, , Feb-28, Volume: 56, Issue:4, 2013
Synthesis and biological evaluation of novel (-)-Cercosporamide derivatives as potent selective PPARγ modulators.European journal of medicinal chemistry, , Volume: 54, 2012
PPARγ agonist from Chromolaena odorata.Journal of natural products, , Dec-28, Volume: 75, Issue:12, 2012
Synthesis, characterization and biological evaluation of ureidofibrate-like derivatives endowed with peroxisome proliferator-activated receptor activity.Journal of medicinal chemistry, , Jan-12, Volume: 55, Issue:1, 2012
Plakilactones from the marine sponge Plakinastrella mamillaris. Discovery of a new class of marine ligands of peroxisome proliferator-activated receptor γ.Journal of medicinal chemistry, , Oct-11, Volume: 55, Issue:19, 2012
Integrated virtual screening for the identification of novel and selective peroxisome proliferator-activated receptor (PPAR) scaffolds.Journal of medicinal chemistry, , Jun-14, Volume: 55, Issue:11, 2012
Substituents at the naphthalene C3 position of (-)-Cercosporamide derivatives significantly affect the maximal efficacy as PPARγ partial agonists.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 22, Issue:3, 2012
Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.Bioorganic & medicinal chemistry, , Jan-15, Volume: 20, Issue:2, 2012
Identification of diaryl ether-based ligands for estrogen-related receptor α as potential antidiabetic agents.Journal of medicinal chemistry, , Feb-10, Volume: 54, Issue:3, 2011
Synthesis, molecular modeling studies and biological evaluation of fluorine substituted analogs of GW 501516.Bioorganic & medicinal chemistry, , Dec-01, Volume: 19, Issue:23, 2011
Discovery of new nanomolar peroxisome proliferator-activated receptor γ activators via elaborate ligand-based modeling.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
Revisiting glitazars: thiophene substituted oxazole containing α-ethoxy phenylpropanoic acid derivatives as highly potent PPARα/γ dual agonists devoid of adverse effects in rodents.Bioorganic & medicinal chemistry letters, , May-15, Volume: 21, Issue:10, 2011
Design, synthesis, and structural analysis of phenylpropanoic acid-type PPARγ-selective agonists: discovery of reversed stereochemistry-activity relationship.Journal of medicinal chemistry, , Jan-13, Volume: 54, Issue:1, 2011
Biological evaluation of novel benzisoxazole derivatives as PPARδ agonists.Bioorganic & medicinal chemistry, , May-15, Volume: 19, Issue:10, 2011
Synthesis of a novel human PPARδ selective agonist and its stimulatory effect on oligodendrocyte differentiation.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.Journal of medicinal chemistry, , Dec-22, Volume: 54, Issue:24, 2011
SAR studies of acidic dual γ-secretase/PPARγ modulators.Bioorganic & medicinal chemistry, , Sep-15, Volume: 19, Issue:18, 2011
Synthesis of new 8(S)-HETE analogs and their biological evaluation as activators of the PPAR nuclear receptors.Journal of enzyme inhibition and medicinal chemistry, , Volume: 25, Issue:5, 2010
Design, synthesis, and structure-activity relationship studies of novel 2,4,6-trisubstituted-5-pyrimidinecarboxylic acids as peroxisome proliferator-activated receptor gamma (PPARgamma) partial agonists with comparable antidiabetic efficacy to rosiglitazoJournal of medicinal chemistry, , Jul-08, Volume: 53, Issue:13, 2010
Identification of (beta-carboxyethyl)-rhodanine derivatives exhibiting peroxisome proliferator-activated receptor gamma activity.European journal of medicinal chemistry, , Volume: 45, Issue:1, 2010
1,3-Diphenyl-1H-pyrazole derivatives as a new series of potent PPARγ partial agonists.Bioorganic & medicinal chemistry, , Dec-01, Volume: 18, Issue:23, 2010
Discovery of a novel selective PPARgamma modulator from (-)-Cercosporamide derivatives.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 20, Issue:7, 2010
(S)-3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-(piperazin-1-yl) propanoic acid compounds: synthesis and biological evaluation of dual PPARalpha/gamma agonists.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
Flexible ligand recognition of peroxisome proliferator-activated receptor-gamma (PPARgamma).Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 20, Issue:11, 2010
Acidic elements in histamine H(3) receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, Issue:5, 2010
Selective, potent PPARgamma agonists with cyclopentenone core structure.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 19, Issue:7, 2009
Design and structural analysis of novel pharmacophores for potent and selective peroxisome proliferator-activated receptor gamma agonists.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists.Bioorganic & medicinal chemistry, , Oct-15, Volume: 17, Issue:20, 2009
New 2-aryloxy-3-phenyl-propanoic acids as peroxisome proliferator-activated receptors alpha/gamma dual agonists with improved potency and reduced adverse effects on skeletal muscle function.Journal of medicinal chemistry, , Oct-22, Volume: 52, Issue:20, 2009
7-Hydroxy-benzopyran-4-one derivatives: a novel pharmacophore of peroxisome proliferator-activated receptor alpha and -gamma (PPARalpha and gamma) dual agonists.Journal of medicinal chemistry, , Nov-12, Volume: 52, Issue:21, 2009
Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes.Bioorganic & medicinal chemistry, , Aug-01, Volume: 17, Issue:15, 2009
Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.Bioorganic & medicinal chemistry letters, , May-01, Volume: 19, Issue:9, 2009
Activation of peroxisome proliferator-activated receptor gamma (PPARgamma) by nitroalkene fatty acids: importance of nitration position and degree of unsaturation.Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
Design, synthesis and insulin-sensitizing activity of indomethacin and diclofenac derivatives.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 19, Issue:12, 2009
Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.Journal of medicinal chemistry, , Jul-23, Volume: 52, Issue:14, 2009
Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus wJournal of medicinal chemistry, , Jul-09, Volume: 52, Issue:13, 2009
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 18, Issue:5, 2008
Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 2008
Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
Design, synthesis, and biological evaluation of novel constrained meta-substituted phenyl propanoic acids as peroxisome proliferator-activated receptor alpha and gamma dual agonists.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies.Bioorganic & medicinal chemistry, , May-01, Volume: 16, Issue:9, 2008
Synthesis and evaluation of a series of benzopyran derivatives as PPAR alpha/gamma agonists.European journal of medicinal chemistry, , Volume: 43, Issue:11, 2008
Discovery of azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 18, Issue:6, 2008
Novel selective PPARdelta agonists: optimization of activity by modification of alkynylallylic moiety.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 17, Issue:15, 2007
Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARalpha/gamma dual agonists.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 17, Issue:13, 2007
Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 17, Issue:4, 2007
Synthesis and structure-activity relationship of novel indene N-oxide derivatives as potent peroxisome proliferator activated receptor gamma (PPARgamma) agonists.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 17, Issue:18, 2007
Design of a partial PPARdelta agonist.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 17, Issue:16, 2007
Design of potent PPARalpha agonists.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 17, Issue:11, 2007
Design and synthesis of indane-ureido-thioisobutyric acids: A novel class of PPARalpha agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 17, Issue:24, 2007
Design and synthesis of novel and potent amide linked PPARgamma/delta dual agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 17, Issue:24, 2007
Design and synthesis of a novel class of dual PPARgamma/delta agonists.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 17, Issue:4, 2007
Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 17, Issue:8, 2007
Insights into the mechanism of partial agonism: crystal structures of the peroxisome proliferator-activated receptor gamma ligand-binding domain in the complex with two enantiomeric ligands.The Journal of biological chemistry, , Jun-08, Volume: 282, Issue:23, 2007
Indol-1-yl acetic acids as peroxisome proliferator-activated receptor agonists: design, synthesis, structural biology, and molecular docking studies.Journal of medicinal chemistry, , Feb-09, Volume: 49, Issue:3, 2006
Design and synthesis of novel N-sulfonyl-2-indole carboxamides as potent PPAR-gamma binding agents with potential application to the treatment of osteoporosis.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 16, Issue:21, 2006
Structure-based de novo design, synthesis, and biological evaluation of the indole-based PPARgamma ligands (I).Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 16, Issue:22, 2006
Tetrahydroisoquinoline PPARgamma agonists: design of novel, highly selective non-TZD antihyperglycemic agents.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 16, Issue:24, 2006
Structural basis for the structure-activity relationships of peroxisome proliferator-activated receptor agonists.Journal of medicinal chemistry, , Oct-19, Volume: 49, Issue:21, 2006
Indenone derivatives: a novel template for peroxisome proliferator-activated receptor gamma (PPARgamma) agonists.Journal of medicinal chemistry, , Jul-27, Volume: 49, Issue:15, 2006
Design and synthesis of the first generation of dithiolane thiazolidinedione- and phenylacetic acid-based PPARgamma agonists.Journal of medicinal chemistry, , Jul-13, Volume: 49, Issue:14, 2006
Synthesis and evaluation of aminomethyl dihydrocinnamates as a new class of PPAR ligands.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 16, Issue:24, 2006
Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 16, Issue:23, 2006
Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 16, Issue:23, 2006
Design and synthesis of dual peroxisome proliferator-activated receptors gamma and delta agonists as novel euglycemic agents with a reduced weight gain profile.Journal of medicinal chemistry, , Sep-21, Volume: 49, Issue:19, 2006
Benzoyl 2-methyl indoles as selective PPARgamma modulators.Bioorganic & medicinal chemistry letters, , Jan-17, Volume: 15, Issue:2, 2005
Discovery of a novel series of peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes and dyslipidemia.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARalpha and PPARgamma agonist activity.Journal of medicinal chemistry, , Aug-25, Volume: 48, Issue:17, 2005
Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARgamma partial agonists.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 15, Issue:22, 2005
Synthesis of new carbo- and heterocyclic analogues of 8-HETE and evaluation of their activity towards the PPARs.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 15, Issue:20, 2005
Selective PPARgamma modulators with improved pharmacological profiles.Bioorganic & medicinal chemistry letters, , May-16, Volume: 15, Issue:10, 2005
2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents.Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 15, Issue:1, 2005
Novel indole-based peroxisome proliferator-activated receptor agonists: design, SAR, structural biology, and biological activities.Journal of medicinal chemistry, , Dec-29, Volume: 48, Issue:26, 2005
Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose andJournal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
(2R)-2-ethylchromane-2-carboxylic acids: discovery of novel PPARalpha/gamma dual agonists as antihyperglycemic and hypolipidemic agents.Journal of medicinal chemistry, , Jun-03, Volume: 47, Issue:12, 2004
Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPARalpha selective activators.Bioorganic & medicinal chemistry letters, , Jul-05, Volume: 14, Issue:13, 2004
Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 2004
Benzoxazinones as PPARgamma agonists. 2. SAR of the amide substituent and in vivo results in a type 2 diabetes model.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template.Bioorganic & medicinal chemistry letters, , Jan-20, Volume: 13, Issue:2, 2003
Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.Bioorganic & medicinal chemistry letters, , Aug-18, Volume: 13, Issue:16, 2003
Amphipathic 3-phenyl-7-propylbenzisoxazoles; human pPaR gamma, delta and alpha agonists.Bioorganic & medicinal chemistry letters, , Mar-10, Volume: 13, Issue:5, 2003
Phenylacetic acid derivatives as hPPAR agonists.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 13, Issue:7, 2003
Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.Journal of medicinal chemistry, , Nov-06, Volume: 46, Issue:23, 2003
Benzoxazinones as PPARgamma agonists. part 1: SAR of three aromatic regions.Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 13, Issue:14, 2003
5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.Bioorganic & medicinal chemistry letters, , May-19, Volume: 13, Issue:10, 2003
Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.Journal of medicinal chemistry, , Feb-14, Volume: 45, Issue:4, 2002
Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists.Journal of medicinal chemistry, , Jun-21, Volume: 44, Issue:13, 2001
Synthesis and biological activity of L-tyrosine-based PPARgamma agonists with reduced molecular weight.Bioorganic & medicinal chemistry letters, , Dec-17, Volume: 11, Issue:24, 2001
The PPARs: from orphan receptors to drug discovery.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
Synthesis and biological activity of a novel series of indole-derived PPARgamma agonists.Bioorganic & medicinal chemistry letters, , Dec-06, Volume: 9, Issue:23, 1999
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents.Journal of medicinal chemistry, , Dec-03, Volume: 41, Issue:25, 1998
Design, synthesis and evaluation of novel zwitterionic compounds as PPARα/γ dual agonists (1).Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
Biological evaluation of novel benzisoxazole derivatives as PPARδ agonists.Bioorganic & medicinal chemistry, , May-15, Volume: 19, Issue:10, 2011
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 2004
Design, synthesis, and evaluation of substituted phenylpropanoic acid derivatives as human peroxisome proliferator activated receptor activators. Discovery of potent and human peroxisome proliferator activated receptor alpha subtype-selective activators.Journal of medicinal chemistry, , Aug-14, Volume: 46, Issue:17, 2003
Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Design, synthesis and evaluation of substituted phenylpropanoic acid derivatives as peroxisome proliferator-activated receptor (PPAR) activators: novel human PPARalpha-selective activators.Bioorganic & medicinal chemistry letters, , Jan-07, Volume: 12, Issue:1, 2002
Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists.Journal of medicinal chemistry, , Jun-21, Volume: 44, Issue:13, 2001
The PPARs: from orphan receptors to drug discovery.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
(3-substituted benzyl)thiazolidine-2,4-diones as structurally new antihyperglycemic agents.Bioorganic & medicinal chemistry letters, , Feb-22, Volume: 9, Issue:4, 1999
Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPARalpha selective activators.Bioorganic & medicinal chemistry letters, , Jul-05, Volume: 14, Issue:13, 2004
The PPARs: from orphan receptors to drug discovery.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
Anti-diabetic activity of fused PPARγ-SIRT1 ligands with limited body-weight gain by mimicking calorie restriction and decreasing SGK1 expression.European journal of medicinal chemistry, , Sep-08, Volume: 137, 2017
Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.Journal of medicinal chemistry, , Dec-22, Volume: 54, Issue:24, 2011
Flexible ligand recognition of peroxisome proliferator-activated receptor-gamma (PPARgamma).Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 20, Issue:11, 2010
QSAR analysis of PPAR-gamma agonists as anti-diabetic agents.European journal of medicinal chemistry, , Volume: 43, Issue:1, 2008
Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 17, Issue:8, 2007
Tetrahydroisoquinoline PPARgamma agonists: design of novel, highly selective non-TZD antihyperglycemic agents.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 16, Issue:24, 2006
Synthesis and biological activity of L-tyrosine-based PPARgamma agonists with reduced molecular weight.Bioorganic & medicinal chemistry letters, , Dec-17, Volume: 11, Issue:24, 2001
The PPARs: from orphan receptors to drug discovery.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 3. Structure-activity relationship and optimization of the N-aryl substituent.Journal of medicinal chemistry, , Dec-03, Volume: 41, Issue:25, 1998
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 2. Structure-activity relationship and optimization of the phenyl alkyl ether moiety.Journal of medicinal chemistry, , Dec-03, Volume: 41, Issue:25, 1998
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents.Journal of medicinal chemistry, , Dec-03, Volume: 41, Issue:25, 1998
PPARγ-sparing thiazolidinediones as insulin sensitizers. Design, synthesis and selection of compounds for clinical development.Bioorganic & medicinal chemistry, , 12-01, Volume: 26, Issue:22, 2018
Anti-diabetic activity of fused PPARγ-SIRT1 ligands with limited body-weight gain by mimicking calorie restriction and decreasing SGK1 expression.European journal of medicinal chemistry, , Sep-08, Volume: 137, 2017
Synthesis and biological evaluation of novel pyrrolidine acid analogs as potent dual PPARα/γ agonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 25, Issue:6, 2015
Design, synthesis and evaluation of novel zwitterionic compounds as PPARα/γ dual agonists (1).Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
Design, synthesis and structure-activity relationships of azole acids as novel, potent dual PPAR alpha/gamma agonists.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 19, Issue:5, 2009
Modulation of PPAR receptor subtype selectivity of the ligands: aliphatic chain vs aromatic ring as a spacer between pharmacophore and the lipophilic moiety.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 18, Issue:24, 2008
Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 2008
Design, synthesis, and structure-activity relationships of piperidine and dehydropiperidine carboxylic acids as novel, potent dual PPARalpha/gamma agonists.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 18, Issue:12, 2008
Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose andJournal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 2004
Switching subtype-selectivity: Fragment replacement strategy affords novel class of peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists.Bioorganic & medicinal chemistry letters, , 07-15, Volume: 27, Issue:14, 2017
Design, synthesis and evaluation of novel zwitterionic compounds as PPARα/γ dual agonists (1).Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 18, Issue:5, 2008
Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 2008
Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 18, Issue:20, 2008
Design, synthesis, and biological evaluation of novel constrained meta-substituted phenyl propanoic acids as peroxisome proliferator-activated receptor alpha and gamma dual agonists.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 17, Issue:4, 2007
Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Structure-guided evolution of a 2-phenyl-4-carboxyquinoline chemotype into PPARα selective agonists: New leads for oculovascular conditions.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 28, Issue:16, 2018
(S)-3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-(piperazin-1-yl) propanoic acid compounds: synthesis and biological evaluation of dual PPARalpha/gamma agonists.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
Design, synthesis, biological evaluation and docking studies of pterostilbene analogs inside PPARalpha.Bioorganic & medicinal chemistry, , Apr-01, Volume: 16, Issue:7, 2008
Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 2004
Switching subtype-selectivity: Fragment replacement strategy affords novel class of peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists.Bioorganic & medicinal chemistry letters, , 07-15, Volume: 27, Issue:14, 2017
Design, synthesis and evaluation of novel zwitterionic compounds as PPARα/γ dual agonists (1).Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 2004
Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template.Bioorganic & medicinal chemistry letters, , Jan-20, Volume: 13, Issue:2, 2003
Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.Journal of medicinal chemistry, , Feb-14, Volume: 45, Issue:4, 2002
Mechanistic Insight on the Mode of Action of Colletoic Acid.Journal of medicinal chemistry, , 08-08, Volume: 62, Issue:15, 2019
Tryptophan-containing dipeptide derivatives as potent PPARgamma antagonists: design, synthesis, biological evaluation, and molecular modeling.European journal of medicinal chemistry, , Volume: 43, Issue:12, 2008
Selenium bioisosteric replacement of adenosine derivatives promoting adiponectin secretion increases the binding affinity to peroxisome proliferator-activated receptor δ.Bioorganic & medicinal chemistry, , 01-01, Volume: 28, Issue:1, 2020
Polypharmacology of NJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Structural characterization of amorfrutins bound to the peroxisome proliferator-activated receptor γ.Journal of medicinal chemistry, , Feb-28, Volume: 56, Issue:4, 2013
Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
O-arylmandelic acids as highly selective human PPAR alpha/gamma agonists.Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 13, Issue:19, 2003
Novel oximes having 5-benzyl-2,4-thiazolidinedione as antihyperglycemic agents: synthesis and structure-activity relationship.Bioorganic & medicinal chemistry letters, , Feb-21, Volume: 10, Issue:4, 2000
Identification of dual PPARα/γ agonists and their effects on lipid metabolism.Bioorganic & medicinal chemistry, , Dec-15, Volume: 23, Issue:24, 2015
The discovery of novel isoflavone pan peroxisome proliferator-activated receptor agonists.Bioorganic & medicinal chemistry, , Feb-01, Volume: 21, Issue:3, 2013
7-Hydroxy-benzopyran-4-one derivatives: a novel pharmacophore of peroxisome proliferator-activated receptor alpha and -gamma (PPARalpha and gamma) dual agonists.Journal of medicinal chemistry, , Nov-12, Volume: 52, Issue:21, 2009
Design, synthesis, and biological evaluation of novel sulindac derivatives as partial agonists of PPARγ with potential anti-diabetic efficacy.European journal of medicinal chemistry, , Oct-15, Volume: 222, 2021
Sulindac derivatives that activate the peroxisome proliferator-activated receptor gamma but lack cyclooxygenase inhibition.Journal of medicinal chemistry, , Aug-28, Volume: 51, Issue:16, 2008
Design, Synthesis, and Biological Activity of l-1'-Homologated Adenosine Derivatives.ACS medicinal chemistry letters, , Jul-14, Volume: 13, Issue:7, 2022
Discovery of Pan-peroxisome Proliferator-Activated Receptor Modulators from an Endolichenic Fungus, Journal of natural products, , 12-23, Volume: 85, Issue:12, 2022
Galangin 3-benzyl-5-methylether derivatives function as an adiponectin synthesis-promoting peroxisome proliferator-activated receptor γ partial agonist.Bioorganic & medicinal chemistry, , 01-15, Volume: 54, 2022
[no title available]Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Photohormones Enable Optical Control of the Peroxisome Proliferator-Activated Receptor γ (PPARγ).Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Selenium bioisosteric replacement of adenosine derivatives promoting adiponectin secretion increases the binding affinity to peroxisome proliferator-activated receptor δ.Bioorganic & medicinal chemistry, , 01-01, Volume: 28, Issue:1, 2020
Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool.MedChemComm, , Aug-01, Volume: 10, Issue:8, 2019
Polypharmacology of NJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.Journal of medicinal chemistry, , Oct-13, Volume: 59, Issue:19, 2016
Integrated virtual screening for the identification of novel and selective peroxisome proliferator-activated receptor (PPAR) scaffolds.Journal of medicinal chemistry, , Jun-14, Volume: 55, Issue:11, 2012
Synthesis and biological activities of novel indole derivatives as potent and selective PPARgamma modulators.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 20, Issue:4, 2010
QSAR analysis of PPAR-gamma agonists as anti-diabetic agents.European journal of medicinal chemistry, , Volume: 43, Issue:1, 2008
The PPARs: from orphan receptors to drug discovery.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents.Journal of medicinal chemistry, , Dec-03, Volume: 41, Issue:25, 1998
Studies towards the conception of new selective PPARbeta/delta ligands.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 16, Issue:17, 2006
The PPARs: from orphan receptors to drug discovery.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
The dipeptide H-Trp-Glu-OH (WE) shows agonistic activity to peroxisome proliferator-activated protein-α and reduces hepatic lipid accumulation in lipid-loaded H4IIE cells.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 24, Issue:13, 2014
Tryptophan-containing dipeptide derivatives as potent PPARgamma antagonists: design, synthesis, biological evaluation, and molecular modeling.European journal of medicinal chemistry, , Volume: 43, Issue:12, 2008
Discovery and structure-based design of a new series of potent and selective PPARδ agonists utilizing a virtual screening method.Bioorganic & medicinal chemistry letters, , 03-01, Volume: 59, 2022
Synthesis and evaluation of an orally available "Y"-shaped biaryl peroxisome proliferator-activated receptor δ agonist.Bioorganic & medicinal chemistry, , 08-15, Volume: 26, Issue:15, 2018
Highly selective peroxisome proliferator-activated receptor δ (PPARδ) modulator demonstrates improved safety profile compared to GW501516.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 28, Issue:3, 2018
Activity landscape modeling of PPAR ligands with dual-activity difference maps.Bioorganic & medicinal chemistry, , Jun-01, Volume: 20, Issue:11, 2012
Discovery, design and synthesis of Y-shaped peroxisome proliferator-activated receptor δ agonists as potent anti-obesity agents in vivo.European journal of medicinal chemistry, , Volume: 53, 2012
Synthesis, molecular modeling studies and biological evaluation of fluorine substituted analogs of GW 501516.Bioorganic & medicinal chemistry, , Dec-01, Volume: 19, Issue:23, 2011
Phenoxyacetic acids as PPARδ partial agonists: synthesis, optimization, and in vivo efficacy.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 21, Issue:8, 2011
Biological evaluation of novel benzisoxazole derivatives as PPARδ agonists.Bioorganic & medicinal chemistry, , May-15, Volume: 19, Issue:10, 2011
Effect of structurally constrained oxime-ether linker on PPAR subtype selectivity: Discovery of a novel and potent series of PPAR-pan agonists.Bioorganic & medicinal chemistry, , Jan-15, Volume: 19, Issue:2, 2011
Synthesis of a novel human PPARδ selective agonist and its stimulatory effect on oligodendrocyte differentiation.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
Selective, potent PPARgamma agonists with cyclopentenone core structure.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 19, Issue:7, 2009
Discovery of a novel class of PPARdelta partial agonists.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 2008
Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonists. 1. Discovery of a novel series of potent HDLc raising agents.Journal of medicinal chemistry, , Feb-22, Volume: 50, Issue:4, 2007
Novel selective PPARdelta agonists: optimization of activity by modification of alkynylallylic moiety.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 17, Issue:15, 2007
Design, synthesis, and evaluation of potent, structurally novel peroxisome proliferator-activated receptor (PPAR) delta-selective agonists.Bioorganic & medicinal chemistry, , Aug-01, Volume: 15, Issue:15, 2007
Design of a partial PPARdelta agonist.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 17, Issue:16, 2007
Synthesis and identification of [1,2,4]thiadiazole derivatives as a new series of potent and orally active dual agonists of peroxisome proliferator-activated receptors alpha and delta.Journal of medicinal chemistry, , Aug-09, Volume: 50, Issue:16, 2007
Studies towards the conception of new selective PPARbeta/delta ligands.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 16, Issue:17, 2006
3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists. Part 2.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 16, Issue:21, 2006
3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists: Part 1.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity.Bioorganic & medicinal chemistry letters, , May-05, Volume: 13, Issue:9, 2003
Discovery of new nanomolar peroxisome proliferator-activated receptor γ activators via elaborate ligand-based modeling.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 2004
5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.Bioorganic & medicinal chemistry letters, , Aug-18, Volume: 13, Issue:16, 2003
Aryloxazolidinediones: identification of potent orally active PPAR dual alpha/gamma agonists.Bioorganic & medicinal chemistry letters, , Oct-20, Volume: 13, Issue:20, 2003
Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.Bioorganic & medicinal chemistry, , 10-01, Volume: 26, Issue:18, 2018
[no title available]Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Design and synthesis of fluorinated RXR modulators.Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 13, Issue:19, 2003
Novel (2E,4E,6Z)-7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta-2,4,6-trienoic acid retinoid X receptor modulators are active in models of type 2 diabetes.Journal of medicinal chemistry, , Jun-19, Volume: 46, Issue:13, 2003
[no title available]Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome.European journal of medicinal chemistry, , Dec-05, Volume: 225, 2021
Design, synthesis, and biological evaluation of a novel dual peroxisome proliferator-activated receptor alpha/delta agonist for the treatment of diabetic kidney disease through anti-inflammatory mechanisms.European journal of medicinal chemistry, , Jun-05, Volume: 218, 2021
Discovery of a Novel Selective Dual Peroxisome Proliferator-Activated Receptor α/δ Agonist for the Treatment of Primary Biliary Cirrhosis.ACS medicinal chemistry letters, , Jul-11, Volume: 10, Issue:7, 2019
Glycine amides as PPARalpha agonists.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 20, Issue:11, 2010
Selective, potent PPARgamma agonists with cyclopentenone core structure.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 19, Issue:7, 2009
Design and synthesis of indane-ureido-thioisobutyric acids: A novel class of PPARalpha agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 17, Issue:24, 2007
Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 17, Issue:4, 2007
Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
The PPARs: from orphan receptors to drug discovery.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARalpha agonist with potent lipid-lowering activity.Journal of medicinal chemistry, , Sep-23, Volume: 42, Issue:19, 1999
Co-crystal structure guided array synthesis of PPARgamma inverse agonists.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 17, Issue:14, 2007
Synthesis and biological activity of L-tyrosine-based PPARgamma agonists with reduced molecular weight.Bioorganic & medicinal chemistry letters, , Dec-17, Volume: 11, Issue:24, 2001
The PPARs: from orphan receptors to drug discovery.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 3. Structure-activity relationship and optimization of the N-aryl substituent.Journal of medicinal chemistry, , Dec-03, Volume: 41, Issue:25, 1998
Activity landscape modeling of PPAR ligands with dual-activity difference maps.Bioorganic & medicinal chemistry, , Jun-01, Volume: 20, Issue:11, 2012
Design, synthesis and evaluation of novel zwitterionic compounds as PPARα/γ dual agonists (1).Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents.Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 15, Issue:1, 2005
Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 2004
Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists.Journal of medicinal chemistry, , Jun-21, Volume: 44, Issue:13, 2001
Activity landscape modeling of PPAR ligands with dual-activity difference maps.Bioorganic & medicinal chemistry, , Jun-01, Volume: 20, Issue:11, 2012
Discovery of new nanomolar peroxisome proliferator-activated receptor γ activators via elaborate ligand-based modeling.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
Phenylacetic acid derivatives as hPPAR agonists.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 13, Issue:7, 2003
The PPARs: from orphan receptors to drug discovery.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
Synthesis and Evaluation of PPARδ Agonists That Promote Osteogenesis in a Human Mesenchymal Stem Cell Culture and in a Mouse Model of Human Osteoporosis.Journal of medicinal chemistry, , 05-27, Volume: 64, Issue:10, 2021
Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity.Bioorganic & medicinal chemistry letters, , May-05, Volume: 13, Issue:9, 2003
Activity landscape modeling of PPAR ligands with dual-activity difference maps.Bioorganic & medicinal chemistry, , Jun-01, Volume: 20, Issue:11, 2012
Discovery of new nanomolar peroxisome proliferator-activated receptor γ activators via elaborate ligand-based modeling.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
SAR studies: designing potent and selective LXR agonists.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 16, Issue:11, 2006
Phenylacetic acid derivatives as hPPAR agonists.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 13, Issue:7, 2003
Modulation of PPAR receptor subtype selectivity of the ligands: aliphatic chain vs aromatic ring as a spacer between pharmacophore and the lipophilic moiety.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 18, Issue:24, 2008
Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 18, Issue:20, 2008
Structure-activity studies on 1,3-dioxane-2-carboxylic acid derivatives, a novel class of subtype-selective peroxisome proliferator-activated receptor alpha (PPARalpha) agonists.Bioorganic & medicinal chemistry, , Jan-15, Volume: 16, Issue:2, 2008
Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists.Journal of medicinal chemistry, , Jun-21, Volume: 44, Issue:13, 2001
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents.Journal of medicinal chemistry, , Dec-03, Volume: 41, Issue:25, 1998
Biological evaluation of novel benzisoxazole derivatives as PPARδ agonists.Bioorganic & medicinal chemistry, , May-15, Volume: 19, Issue:10, 2011
Synthesis of a novel human PPARδ selective agonist and its stimulatory effect on oligodendrocyte differentiation.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
The discovery of equipotent PPARalpha/gamma dual activators.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 18, Issue:23, 2008
Design, synthesis and evaluation of trifluoromethane sulfonamide derivatives as new potent and selective peroxisome proliferator-activated receptor alpha agonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonists. 1. Discovery of a novel series of potent HDLc raising agents.Journal of medicinal chemistry, , Feb-22, Volume: 50, Issue:4, 2007
[no title available]Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Structure-Activity Relationship of 2,4-Dichloro-N-(3,5-dichloro-4-(quinolin-3-yloxy)phenyl)benzenesulfonamide (INT131) Analogs for PPARγ-Targeted Antidiabetics.Journal of medicinal chemistry, , 06-08, Volume: 60, Issue:11, 2017
Structure-activity relationship studies of non-carboxylic acid peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists.Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Discovery of INT131: a selective PPARγ modulator that enhances insulin sensitivity.Bioorganic & medicinal chemistry, , Feb-15, Volume: 21, Issue:4, 2013
The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Discovery of para-alkylthiophenoxyacetic acids as a novel series of potent and selective PPARdelta agonists.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 17, Issue:14, 2007
Insights into PPARγ Phosphorylation and Its Inhibition Mechanism.Journal of medicinal chemistry, , 05-14, Volume: 63, Issue:9, 2020
Identification of the First PPARα/γ Dual Agonist Able To Bind to Canonical and Alternative Sites of PPARγ and To Inhibit Its Cdk5-Mediated Phosphorylation.Journal of medicinal chemistry, , 09-27, Volume: 61, Issue:18, 2018
Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175.European journal of medicinal chemistry, , Jan-27, Volume: 90, 2015
Molecular determinants for nuclear receptors selectivity: chemometric analysis, dockings and site-directed mutagenesis of dual peroxisome proliferator-activated receptors α/γ agonists.European journal of medicinal chemistry, , Volume: 63, 2013
New 2-(aryloxy)-3-phenylpropanoic acids as peroxisome proliferator-activated receptor α/γ dual agonists able to upregulate mitochondrial carnitine shuttle system gene expression.Journal of medicinal chemistry, , Jan-10, Volume: 56, Issue:1, 2013
New 2-aryloxy-3-phenyl-propanoic acids as peroxisome proliferator-activated receptors alpha/gamma dual agonists with improved potency and reduced adverse effects on skeletal muscle function.Journal of medicinal chemistry, , Oct-22, Volume: 52, Issue:20, 2009
Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARalpha and PPARgamma agonist activity.Journal of medicinal chemistry, , Aug-25, Volume: 48, Issue:17, 2005
Selenium bioisosteric replacement of adenosine derivatives promoting adiponectin secretion increases the binding affinity to peroxisome proliferator-activated receptor δ.Bioorganic & medicinal chemistry, , 01-01, Volume: 28, Issue:1, 2020
Polypharmacology of NJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
[no title available]Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Peroxisome Proliferator-Activated Receptor γ (PPARγ) and Ligand Choreography: Newcomers Take the Stage.Journal of medicinal chemistry, , Jul-23, Volume: 58, Issue:14, 2015
Discovery of an oxybenzylglycine based peroxisome proliferator activated receptor alpha selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic acid (BMS-687453).Journal of medicinal chemistry, , Apr-08, Volume: 53, Issue:7, 2010
Synthesis and structure-activity relationships of 2-aryl-4-oxazolylmethoxy benzylglycines and 2-aryl-4-thiazolylmethoxy benzylglycines as novel, potent PPARalpha selective activators- PPARalpha and PPARgamma selectivity modulation.Bioorganic & medicinal chemistry letters, , May-01, Volume: 20, Issue:9, 2010
Novel peroxisome proliferator-activated receptor alpha agonists lower low-density lipoprotein and triglycerides, raise high-density lipoprotein, and synergistically increase cholesterol excretion with a liver X receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 327, Issue:3, 2008
Peroxisome Proliferator-Activated Receptor γ (PPARγ) and Ligand Choreography: Newcomers Take the Stage.Journal of medicinal chemistry, , Jul-23, Volume: 58, Issue:14, 2015
Structural characterization of amorfrutins bound to the peroxisome proliferator-activated receptor γ.Journal of medicinal chemistry, , Feb-28, Volume: 56, Issue:4, 2013
Amorfrutins Are Natural PPARγ Agonists with Potent Anti-inflammatory Properties.Journal of natural products, , May-22, Volume: 78, Issue:5, 2015
Structural characterization of amorfrutins bound to the peroxisome proliferator-activated receptor γ.Journal of medicinal chemistry, , Feb-28, Volume: 56, Issue:4, 2013
Identification of pirinixic acid derivatives bearing a 2-aminothiazole moiety combines dual PPARα/γ activation and dual 5-LO/mPGES-1 inhibition.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 24, Issue:16, 2014
Molecular determinants for improved activity at PPARα: structure-activity relationship of pirinixic acid derivatives, docking study and site-directed mutagenesis of PPARα.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 24, Issue:16, 2014
Rational design of a pirinixic acid derivative that acts as subtype-selective PPARgamma modulator.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
Discovery by Virtual Screening of an Inhibitor of CDK5-Mediated PPARγ Phosphorylation.ACS medicinal chemistry letters, , Apr-14, Volume: 13, Issue:4, 2022
Design, Synthesis, and Biological Evaluation of Indole Biphenylcarboxylic Acids as PPARγ Antagonists.ACS medicinal chemistry letters, , Sep-10, Volume: 6, Issue:9, 2015
Activity landscape modeling of PPAR ligands with dual-activity difference maps.Bioorganic & medicinal chemistry, , Jun-01, Volume: 20, Issue:11, 2012
Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Enables
This protein enables 28 target(s):
Target | Category | Definition |
transcription cis-regulatory region binding | molecular function | Binding to a specific sequence of DNA that is part of a regulatory region that controls transcription of that section of the DNA. The transcribed region might be described as a gene, cistron, or operon. [GOC:txnOH] |
RNA polymerase II cis-regulatory region sequence-specific DNA binding | molecular function | Binding to a specific upstream regulatory DNA sequence (transcription factor recognition sequence or binding site) located in cis relative to the transcription start site (i.e., on the same strand of DNA) of a gene transcribed by RNA polymerase II. [GOC:txnOH-2018] |
DNA-binding transcription factor activity, RNA polymerase II-specific | molecular function | A DNA-binding transcription factor activity that modulates the transcription of specific gene sets transcribed by RNA polymerase II. [GOC:txnOH-2018] |
transcription coregulator binding | molecular function | Binding to a transcription coregulator, a protein involved in regulation of transcription via protein-protein interactions with transcription factors and other transcription regulatory proteins. Cofactors do not bind DNA directly, but rather mediate protein-protein interactions between regulatory transcription factors and the basal transcription machinery. [GOC:krc] |
DNA-binding transcription activator activity, RNA polymerase II-specific | molecular function | A DNA-binding transcription factor activity that activates or increases transcription of specific gene sets transcribed by RNA polymerase II. [GOC:aruk, GOC:txnOH-2018, PMID:20737563, PMID:27145859] |
nucleic acid binding | molecular function | Binding to a nucleic acid. [GOC:jl] |
DNA binding | molecular function | Any molecular function by which a gene product interacts selectively and non-covalently with DNA (deoxyribonucleic acid). [GOC:dph, GOC:jl, GOC:tb, GOC:vw] |
chromatin binding | molecular function | Binding to chromatin, the network of fibers of DNA, protein, and sometimes RNA, that make up the chromosomes of the eukaryotic nucleus during interphase. [GOC:jl, ISBN:0198506732, PMID:20404130] |
double-stranded DNA binding | molecular function | Binding to double-stranded DNA. [GOC:elh, GOC:vw] |
DNA-binding transcription factor activity | molecular function | A transcription regulator activity that modulates transcription of gene sets via selective and non-covalent binding to a specific double-stranded genomic DNA sequence (sometimes referred to as a motif) within a cis-regulatory region. Regulatory regions include promoters (proximal and distal) and enhancers. Genes are transcriptional units, and include bacterial operons. [GOC:txnOH-2018] |
nuclear receptor activity | molecular function | A DNA-binding transcription factor activity regulated by binding to a ligand that modulates the transcription of specific gene sets transcribed by RNA polymerase II. Nuclear receptor ligands are usually lipid-based (such as a steroid hormone) and the binding of the ligand to its receptor often occurs in the cytosol, which leads to its translocation to the nucleus. [GOC:txnOH-2018, PMID:23457262] |
prostaglandin receptor activity | molecular function | Combining with a prostaglandin (PG) to initiate a change in cell activity. [ISBN:0198506732] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
enzyme binding | molecular function | Binding to an enzyme, a protein with catalytic activity. [GOC:jl] |
peptide binding | molecular function | Binding to a peptide, an organic compound comprising two or more amino acids linked by peptide bonds. [GOC:jl] |
identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
sequence-specific DNA binding | molecular function | Binding to DNA of a specific nucleotide composition, e.g. GC-rich DNA binding, or with a specific sequence motif or type of DNA e.g. promotor binding or rDNA binding. [GOC:jl] |
nuclear retinoid X receptor binding | molecular function | Binding to a nuclear retinoid X receptor. [GOC:ai] |
arachidonic acid binding | molecular function | Binding to arachidonic acid, a straight chain fatty acid with 20 carbon atoms and four double bonds per molecule. Arachidonic acid is the all-Z-(5,8,11,14)-isomer. [GOC:ai] |
DNA binding domain binding | molecular function | Binding to a protein's DNA binding domain (DBD). [PMID:9682036] |
LBD domain binding | molecular function | Binding to a protein's ligand binding domain (LBD) domain, found in nuclear receptors. In general, the LBDs consist of three layers comprised of twelve alpha-helices and several beta-strands that are organized around a lipophilic ligand-binding pocket. [PMID:9682036] |
alpha-actinin binding | molecular function | Binding to alpha-actinin, one of a family of proteins that cross-link F-actin as antiparallel homodimers. Alpha-actinin has a molecular mass of 93-103 KDa; at the N-terminus there are two calponin homology domains, at the C-terminus there are two EF-hands. These two domains are connected by the rod domain. This domain is formed by triple-helical spectrin repeats. [PMID:10984498, PMID:11699871, PMID:15014165] |
R-SMAD binding | molecular function | Binding to a receptor-regulated SMAD signaling protein. [GOC:BHF, GOC:vk, PMID:19114992] |
E-box binding | molecular function | Binding to an E-box, a DNA motif with the consensus sequence CANNTG that is found in the promoters of a wide array of genes expressed in neurons, muscle and other tissues. [GOC:BHF, GOC:vk, PMID:11812799] |
STAT family protein binding | molecular function | Binding to a member of the signal transducers and activators of transcription (STAT) protein family. STATs are, as the name indicates, both signal transducers and transcription factors. STATs are activated by cytokines and some growth factors and thus control important biological processes including cell growth, cell differentiation, apoptosis and immune responses. [GOC:mr, InterPro:IPR001217, PMID:21447371, PMID:24470978] |
DNA-binding transcription factor binding | molecular function | Binding to a DNA-binding transcription factor, a protein that interacts with a specific DNA sequence (sometimes referred to as a motif) within the regulatory region of a gene to modulate transcription. [GOC:txnOH-2018] |
DNA-binding transcription repressor activity, RNA polymerase II-specific | molecular function | A DNA-binding transcription factor activity that represses or decreases the transcription of specific gene sets transcribed by RNA polymerase II. [GOC:txnOH-2018] |
Located In
This protein is located in 4 target(s):
Target | Category | Definition |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
intracellular membrane-bounded organelle | cellular component | Organized structure of distinctive morphology and function, bounded by a single or double lipid bilayer membrane and occurring within the cell. Includes the nucleus, mitochondria, plastids, vacuoles, and vesicles. Excludes the plasma membrane. [GOC:go_curators] |
Active In
This protein is active in 1 target(s):
Target | Category | Definition |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
Part Of
This protein is part of 3 target(s):
Target | Category | Definition |
RNA polymerase II transcription regulator complex | cellular component | A transcription factor complex that acts at a regulatory region of a gene transcribed by RNA polymerase II. [GOC:tb] |
chromatin | cellular component | The ordered and organized complex of DNA, protein, and sometimes RNA, that forms the chromosome. [GOC:elh, PMID:20404130] |
receptor complex | cellular component | Any protein complex that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:go_curators] |
Involved In
This protein is involved in 61 target(s):
Target | Category | Definition |
negative regulation of transcription by RNA polymerase II | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |
placenta development | biological process | The process whose specific outcome is the progression of the placenta over time, from its formation to the mature structure. The placenta is an organ of metabolic interchange between fetus and mother, partly of embryonic origin and partly of maternal origin. [GOC:add, ISBN:068340007X] |
regulation of transcription by RNA polymerase II | biological process | Any process that modulates the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |
lipid metabolic process | biological process | The chemical reactions and pathways involving lipids, compounds soluble in an organic solvent but not, or sparingly, in an aqueous solvent. Includes fatty acids; neutral fats, other fatty-acid esters, and soaps; long-chain (fatty) alcohols and waxes; sphingoids and other long-chain bases; glycolipids, phospholipids and sphingolipids; and carotenes, polyprenols, sterols, terpenes and other isoprenoids. [GOC:ma] |
activation of cysteine-type endopeptidase activity involved in apoptotic process | biological process | Any process that initiates the activity of the inactive enzyme cysteine-type endopeptidase in the context of an apoptotic process. [GOC:al, GOC:dph, GOC:jl, GOC:mtg_apoptosis, GOC:tb, PMID:14744432, PMID:18328827, Wikipedia:Caspase] |
signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
response to nutrient | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a nutrient stimulus. [GOC:go_curators] |
regulation of blood pressure | biological process | Any process that modulates the force with which blood travels through the circulatory system. The process is controlled by a balance of processes that increase pressure and decrease pressure. [GOC:dph, GOC:mtg_cardio, ISBN:0721643949] |
positive regulation of gene expression | biological process | Any process that increases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
negative regulation of gene expression | biological process | Any process that decreases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
macrophage derived foam cell differentiation | biological process | The process in which a monocyte acquires the specialized features of a foam cell. A foam cell is a type of cell containing lipids in small vacuoles and typically seen in atherosclerotic lesions, as well as other conditions. [GOC:add, GOC:dph, GOC:tb] |
negative regulation of macrophage derived foam cell differentiation | biological process | Any process that decreases the rate, frequency or extent of macrophage derived foam cell differentiation. Macrophage derived foam cell differentiation is the process in which a macrophage acquires the specialized features of a foam cell. A foam cell is a type of cell containing lipids in small vacuoles and typically seen in atherosclerotic lesions, as well as other conditions. [GOC:add, GOC:BHF, GOC:dph, GOC:tb] |
negative regulation of cholesterol storage | biological process | Any process that decreases the rate or extent of cholesterol storage. Cholesterol storage is the accumulation and maintenance in cells or tissues of cholesterol, cholest-5-en-3 beta-ol, the principal sterol of vertebrates and the precursor of many steroids, including bile acids and steroid hormones. [GOC:BHF, GOC:dph, GOC:tb] |
negative regulation of lipid storage | biological process | Any process that decreases the rate, frequency or extent of lipid storage. Lipid storage is the accumulation and maintenance in cells or tissues of lipids, compounds soluble in organic solvents but insoluble or sparingly soluble in aqueous solvents. Lipid reserves can be accumulated during early developmental stages for mobilization and utilization at later stages of development. [GOC:BHF, GOC:dph, GOC:tb] |
negative regulation of sequestering of triglyceride | biological process | Any process that decreases the rate, frequency or extent of sequestering of triglyceride. Triglyceride sequestration is the process of binding or confining any triester of glycerol such that it is separated from other components of a biological system. [GOC:BHF, GOC:dph, GOC:tb] |
negative regulation of angiogenesis | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of angiogenesis. [GOC:go_curators] |
monocyte differentiation | biological process | The process in which a relatively unspecialized myeloid precursor cell acquires the specialized features of a monocyte. [GOC:mah] |
BMP signaling pathway | biological process | The series of molecular signals initiated by the binding of a member of the BMP (bone morphogenetic protein) family to a receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:signaling, ISBN:0878932437, PMID:17428827] |
negative regulation of transforming growth factor beta receptor signaling pathway | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of any TGF-beta receptor signaling pathway. [GOC:mah] |
epithelial cell differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized features of an epithelial cell, any of the cells making up an epithelium. [GOC:ecd, PMID:11839751] |
cellular response to insulin stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an insulin stimulus. Insulin is a polypeptide hormone produced by the islets of Langerhans of the pancreas in mammals, and by the homologous organs of other organisms. [GOC:mah, ISBN:0198506732] |
response to lipid | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipid stimulus. [GOC:sl] |
peroxisome proliferator activated receptor signaling pathway | biological process | The series of molecular signals initiated by binding of a ligand to any of the peroxisome proliferator activated receptors (alpha, beta or gamma) in the nuclear membrane, and ending with the initiation or termination of the transcription of target genes. [GOC:BHF, PMID:18221086] |
glucose homeostasis | biological process | Any process involved in the maintenance of an internal steady state of glucose within an organism or cell. [GOC:go_curators] |
regulation of circadian rhythm | biological process | Any process that modulates the frequency, rate or extent of a circadian rhythm. A circadian rhythm is a biological process in an organism that recurs with a regularity of approximately 24 hours. [GOC:dph, GOC:jl, GOC:tb] |
mRNA transcription by RNA polymerase II | biological process | The cellular synthesis of messenger RNA (mRNA) from a DNA template by RNA polymerase II, originating at an RNA polymerase II promoter. [GOC:jl, ISBN:0321000382] |
lipoprotein transport | biological process | The directed movement of any conjugated, water-soluble protein in which the nonprotein group consists of a lipid or lipids, into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:jl, ISBN:0198506732] |
negative regulation of blood vessel endothelial cell migration | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the migration of the endothelial cells of blood vessels. [GOC:go_curators] |
innate immune response | biological process | Innate immune responses are defense responses mediated by germline encoded components that directly recognize components of potential pathogens. [GO_REF:0000022, GOC:add, GOC:ebc, GOC:mtg_sensu] |
cell fate commitment | biological process | The cellular developmental process by which a cell establishes the intrinsic character of a cell or tissue region irreversibly committing it to a particular fate. [ISBN:0716731185] |
positive regulation of fat cell differentiation | biological process | Any process that activates or increases the frequency, rate or extent of adipocyte differentiation. [GOC:go_curators] |
negative regulation of DNA-templated transcription | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
positive regulation of DNA-templated transcription | biological process | Any process that activates or increases the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
positive regulation of transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
retinoic acid receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of a retinoic acid receptor binding to one of its physiological ligands. [GOC:dgh] |
cell maturation | biological process | The cellular developmental process, independent of morphogenetic (shape) change, that is required for a specific cell to attain its fully functional state. [GOC:go_curators] |
rhythmic process | biological process | Any process pertinent to the generation and maintenance of rhythms in the physiology of an organism. [GOC:jid] |
white fat cell differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized features of a white adipocyte, an animal connective tissue cell involved in energy storage. White adipocytes have cytoplasmic lipids arranged in a unique vacuole. [PMID:12508945] |
positive regulation of DNA-binding transcription factor activity | biological process | Any process that activates or increases the frequency, rate or extent of activity of a transcription factor, any factor involved in the initiation or regulation of transcription. [GOC:ai] |
lipid homeostasis | biological process | Any process involved in the maintenance of an internal steady state of lipid within an organism or cell. [GOC:BHF, GOC:rl] |
negative regulation of type II interferon-mediated signaling pathway | biological process | Any process that decreases the rate, frequency or extent of an interferon-gamma-mediated signaling pathway. [GOC:dph] |
negative regulation of SMAD protein signal transduction | biological process | Any process that decreases the rate, frequency or extent of the SMAD protein signaling pathway. [GOC:BHF, GOC:dph, GOC:tb] |
regulation of cholesterol transporter activity | biological process | Any process that modulates the rate, frequency, or extent of cholesterol transporter activity. [GOC:BHF, GOC:dph, GOC:tb] |
cellular response to low-density lipoprotein particle stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a low-density lipoprotein particle stimulus. [GOC:mah] |
cellular response to hypoxia | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating lowered oxygen tension. Hypoxia, defined as a decline in O2 levels below normoxic levels of 20.8 - 20.95%, results in metabolic adaptation at both the cellular and organismal level. [GOC:mah] |
negative regulation of mitochondrial fission | biological process | Any process that decreases the rate, frequency or extent of mitochondrial fission. Mitochondrial fission is the division of a mitochondrion within a cell to form two or more separate mitochondrial compartments. [GOC:sl, GOC:tb] |
regulation of cellular response to insulin stimulus | biological process | Any process that modulates the frequency, rate or extent of cellular response to insulin stimulus. [GOC:TermGenie, GOC:yaf] |
negative regulation of extracellular matrix assembly | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of extracellular matrix assembly. [GOC:BHF, GOC:TermGenie] |
negative regulation of miRNA transcription | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of microRNA (miRNA) gene transcription. [GO_REF:0000058, GOC:dph, GOC:kmv, GOC:TermGenie, PMID:24699545] |
positive regulation of miRNA transcription | biological process | Any process that activates or increases the frequency, rate or extent of microRNA (miRNA) gene transcription. [GO_REF:0000058, GOC:dph, GOC:kmv, GOC:TermGenie, PMID:24699545] |
negative regulation of cellular response to transforming growth factor beta stimulus | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of cellular response to transforming growth factor beta stimulus. [GO_REF:0000058, GOC:BHF, GOC:BHF_miRNA, GOC:rph, GOC:TermGenie, PMID:22269326] |
positive regulation of adipose tissue development | biological process | Any process that activates or increases the frequency, rate or extent of adipose tissue development. [GO_REF:0000058, GOC:TermGenie, PMID:23081848] |
negative regulation of vascular associated smooth muscle cell proliferation | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of vascular smooth muscle cell proliferation. [GO_REF:0000058, GOC:TermGenie, PMID:23246467] |
positive regulation of vascular associated smooth muscle cell apoptotic process | biological process | Any process that activates or increases the frequency, rate or extent of vascular associated smooth muscle cell apoptotic process. [GO_REF:0000058, GOC:BHF, GOC:BHF_miRNA, GOC:rph, GOC:TermGenie, PMID:26493107] |
negative regulation of vascular endothelial cell proliferation | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of vascular endothelial cell proliferation. [GO_REF:0000058, GOC:BHF, GOC:BHF_telomere, GOC:nc, GOC:TermGenie, PMID:23201774] |
positive regulation of fatty acid metabolic process | biological process | Any process that activates or increases the frequency, rate or extent of the chemical reactions and pathways involving fatty acids. [GOC:go_curators] |
fatty acid metabolic process | biological process | The chemical reactions and pathways involving fatty acids, aliphatic monocarboxylic acids liberated from naturally occurring fats and oils by hydrolysis. [ISBN:0198547684] |
negative regulation of inflammatory response | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the inflammatory response. [GOC:ai] |
cell differentiation | biological process | The cellular developmental process in which a relatively unspecialized cell, e.g. embryonic or regenerative cell, acquires specialized structural and/or functional features that characterize a specific cell. Differentiation includes the processes involved in commitment of a cell to a specific fate and its subsequent development to the mature state. [ISBN:0198506732] |
hormone-mediated signaling pathway | biological process | The series of molecular signals mediated by the detection of a hormone. [GOC:sm] |