Proteins > Peroxisome proliferator-activated receptor alpha
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Peroxisome proliferator-activated receptor alpha
A peroxisome proliferator-activated receptor alpha that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q07869]
Synonyms
PPAR-alpha;
Nuclear receptor subfamily 1 group C member 1
Research
Bioassay Publications (186)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 5 (2.69) | 18.2507 |
2000's | 87 (46.77) | 29.6817 |
2010's | 79 (42.47) | 24.3611 |
2020's | 15 (8.06) | 2.80 |
Compounds (124)
Drugs with Potency Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
palmitic acid | Homo sapiens (human) | Potency | 17.7828 | 1 | 0 |
2,4,6-tribromophenol | Homo sapiens (human) | Potency | 37.6460 | 1 | 0 |
N-(4-hydroxyphenyl)-3,7-dimethyl-9-(2,6,6-trimethyl-1-cyclohexenyl)nona-2,4,6,8-tetraenamide | Homo sapiens (human) | Potency | 8.9125 | 1 | 0 |
bithionol | Homo sapiens (human) | Potency | 26.6514 | 1 | 0 |
ciglitazone | Homo sapiens (human) | Potency | 44.6684 | 1 | 0 |
ciprofibrate | Homo sapiens (human) | Potency | 14.1254 | 1 | 0 |
dichlorophen | Homo sapiens (human) | Potency | 39.8107 | 1 | 0 |
endosulfan | Homo sapiens (human) | Potency | 44.6684 | 1 | 0 |
flufenamic acid | Homo sapiens (human) | Potency | 28.1838 | 1 | 0 |
gossypol | Homo sapiens (human) | Potency | 15.8489 | 1 | 0 |
mefenamic acid | Homo sapiens (human) | Potency | 35.4813 | 1 | 0 |
mitotane | Homo sapiens (human) | Potency | 39.8107 | 1 | 0 |
chlordan | Homo sapiens (human) | Potency | 31.6228 | 1 | 0 |
2,3,4,6-tetrachlorophenol | Homo sapiens (human) | Potency | 44.6684 | 1 | 0 |
dichlorodiphenyldichloroethane | Homo sapiens (human) | Potency | 50.1187 | 1 | 0 |
1-naphthylphenylamine | Homo sapiens (human) | Potency | 50.1187 | 1 | 0 |
2-phenylphenol | Homo sapiens (human) | Potency | 251.1890 | 1 | 0 |
4,4'-thiobis(6-tert-butyl-3-cresol) | Homo sapiens (human) | Potency | 7.8435 | 1 | 0 |
trans-4-tert-butylcyclohexanol | Homo sapiens (human) | Potency | 1.1220 | 1 | 0 |
12-hydroxy stearic acid | Homo sapiens (human) | Potency | 31.6228 | 1 | 0 |
dicofol | Homo sapiens (human) | Potency | 31.6228 | 1 | 0 |
2,2'-methylenebis(4-methyl-6-tert-butylphenol) | Homo sapiens (human) | Potency | 14.1254 | 1 | 0 |
2-Phenylethyl 2-aminobenzoate | Homo sapiens (human) | Potency | 2.5119 | 1 | 0 |
4-tert-octylphenol | Homo sapiens (human) | Potency | 25.1189 | 1 | 0 |
myristic acid | Homo sapiens (human) | Potency | 33.5278 | 1 | 0 |
allethrins | Homo sapiens (human) | Potency | 50.1187 | 1 | 0 |
o,p'-ddt | Homo sapiens (human) | Potency | 50.1187 | 1 | 0 |
heptachlor epoxide | Homo sapiens (human) | Potency | 50.1187 | 1 | 0 |
antimycin a | Homo sapiens (human) | Potency | 35.4813 | 1 | 0 |
ioxynil | Homo sapiens (human) | Potency | 15.8489 | 1 | 0 |
bromoxynil | Homo sapiens (human) | Potency | 25.1189 | 1 | 0 |
bromoxynil octanoate | Homo sapiens (human) | Potency | 44.6684 | 1 | 0 |
(2-hydroxy-4-(octyloxy)phenyl)phenylmethanone | Homo sapiens (human) | Potency | 44.6684 | 1 | 0 |
4-(octyloxy)benzoic acid | Homo sapiens (human) | Potency | 7.0795 | 1 | 0 |
gamma-glycidoxypropyltrimethoxysilane | Homo sapiens (human) | Potency | 39.8107 | 1 | 0 |
bromotriethylstannane | Homo sapiens (human) | Potency | 5.0119 | 1 | 0 |
mono-(2-ethylhexyl)phthalate | Homo sapiens (human) | Potency | 31.8326 | 1 | 0 |
isostearate | Homo sapiens (human) | Potency | 39.8107 | 1 | 0 |
isopropyl 4,4'-dibromobenzilate | Homo sapiens (human) | Potency | 31.6228 | 1 | 0 |
butylated hydroxytoluene | Homo sapiens (human) | Potency | 39.8107 | 1 | 0 |
amitraz | Homo sapiens (human) | Potency | 39.8107 | 1 | 0 |
oxyfluorofen | Homo sapiens (human) | Potency | 50.1187 | 1 | 0 |
dichlorfop-methyl | Homo sapiens (human) | Potency | 44.6684 | 1 | 0 |
imazethapyr | Homo sapiens (human) | Potency | 39.8107 | 1 | 0 |
lactofen | Homo sapiens (human) | Potency | 35.4813 | 1 | 0 |
1-(diiodomethyl)sulfonyl-4-methyl benzene | Homo sapiens (human) | Potency | 28.1838 | 1 | 0 |
perfluorooctanesulfonamide | Homo sapiens (human) | Potency | 44.6684 | 1 | 0 |
2-bromopalmitate | Homo sapiens (human) | Potency | 14.1254 | 1 | 0 |
4-chloro-n-((4-(1,1-dimethylethyl)phenyl)methyl)-3-ethyl-1-methyl-1h-pyrazole-5-carboxamide | Homo sapiens (human) | Potency | 39.8107 | 1 | 0 |
1-(carboxymethylthio)tetradecane | Homo sapiens (human) | Potency | 10.0000 | 1 | 0 |
lanosterol | Homo sapiens (human) | Potency | 12.5893 | 1 | 0 |
oleic acid | Homo sapiens (human) | Potency | 35.4813 | 1 | 0 |
tamoxifen citrate | Homo sapiens (human) | Potency | 50.1187 | 1 | 0 |
azoxystrobin | Homo sapiens (human) | Potency | 19.9526 | 1 | 0 |
gw 7647 | Homo sapiens (human) | Potency | 0.0158 | 1 | 0 |
sodium dodecyl sulfate | Homo sapiens (human) | Potency | 44.6684 | 1 | 0 |
linoleic acid | Homo sapiens (human) | Potency | 36.4261 | 1 | 0 |
4-(2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-1-propenyl)benzoic acid | Homo sapiens (human) | Potency | 44.6684 | 1 | 0 |
methylbenzethonium chloride | Homo sapiens (human) | Potency | 25.1189 | 1 | 0 |
l-165041 | Homo sapiens (human) | Potency | 11.2202 | 1 | 0 |
6-(4-chlorophenyl)imidazo(2,1-b)(1,3)thiazole-5-carbaldehyde o-(3,4-dichlorobenzyl)oxime | Homo sapiens (human) | Potency | 35.4813 | 1 | 0 |
sorbitan monooleate | Homo sapiens (human) | Potency | 39.8107 | 1 | 0 |
gw0742 | Homo sapiens (human) | Potency | 1.9953 | 1 | 0 |
mesosulfuron-methyl | Homo sapiens (human) | Potency | 35.4813 | 1 | 0 |
sarkosyl | Homo sapiens (human) | Potency | 39.8107 | 1 | 0 |
docusate sodium | Homo sapiens (human) | Potency | 50.1187 | 1 | 0 |
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
troglitazone | Homo sapiens (human) | Fold activation | 1.1200 | 1 | 1 |
farglitazar | Homo sapiens (human) | Log Ki | 6.3100 | 1 | 1 |
gw 1929 | Homo sapiens (human) | Log Ki | 5.5000 | 1 | 1 |
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
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
[no title available],
Targeting peroxisome proliferator-activated receptors (PPARs): development of modulators.Journal of medicinal chemistry, , May-10, Volume: 55, Issue:9, 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
The PPARs: from orphan receptors to drug discovery.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
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
Fibrate-derived N-(methylsulfonyl)amides with antagonistic properties on PPARα.European journal of medicinal chemistry, , Volume: 58, 2012
Synthesis and structure-activity relationships of fibrate-based analogues inside PPARs.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 22, Issue:24, 2012
Benzothiazole-based N-(phenylsulfonyl)amides as a novel family of PPARα antagonists.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 21, Issue:16, 2011
Synthesis and biological evaluation of 2-heteroarylthioalkanoic acid analogues of clofibric acid as peroxisome proliferator-activated receptor alpha agonists.Journal of medicinal chemistry, , Oct-22, Volume: 52, Issue:20, 2009
Phenoxy herbicides and fibrates potently inhibit the human chemosensory receptor subunit T1R3.Journal of medicinal chemistry, , Nov-12, Volume: 52, Issue:21, 2009
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
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
Structural development of 1H-pyrazolo-[3,4-b]pyridine-4-carboxylic acid derivatives as human peroxisome proliferator-activated receptor alpha (PPARα)-selective agonists.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 29, Issue:16, 2019
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
The discovery of novel isoflavone pan peroxisome proliferator-activated receptor agonists.Bioorganic & medicinal chemistry, , Feb-01, Volume: 21, Issue:3, 2013
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
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 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
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
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
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
Discovery of gemfibrozil analogues that activate PPARα and enhance the expression of gene CPT1A involved in fatty acids catabolism.European journal of medicinal chemistry, , Volume: 46, Issue:10, 2011
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
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
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
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
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
Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation.Journal of medicinal chemistry, , 02-28, Volume: 62, Issue:4, 2019
2-Phenyl-8-(1-phenylallyl)-chromenone compounds have a pan-PPAR modulator pharmacophore.Bioorganic & medicinal chemistry, , 07-01, Volume: 27, Issue:13, 2019
[no title available]Journal of natural products, , 07-26, Volume: 82, Issue:7, 2019
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
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
Kojyl cinnamate esters are peroxisome proliferator-activated receptor α/γ dual agonists.Bioorganic & medicinal chemistry, , 11-15, Volume: 26, Issue:21, 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
Structural development studies of PPARs ligands based on tyrosine scaffold.European journal of medicinal chemistry, , Jan-07, Volume: 89, 2015
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
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
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
The discovery of novel isoflavone pan peroxisome proliferator-activated receptor agonists.Bioorganic & medicinal chemistry, , Feb-01, Volume: 21, Issue:3, 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, 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
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
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
Discovery of Potent Dual PPARα Agonists/CB1 Ligands.ACS medicinal chemistry letters, , Nov-10, Volume: 2, Issue:11, 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 docking studies of novel benzimidazoles for the treatment of metabolic syndrome.Journal of medicinal chemistry, , Feb-11, Volume: 53, Issue:3, 2010
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
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
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 and evaluation of a series of benzopyran derivatives as PPAR alpha/gamma agonists.European journal of medicinal chemistry, , Volume: 43, Issue:11, 2008
Novel sulfamide analogs of oleoylethanolamide showing in vivo satiety inducing actions and PPARalpha activation.Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
Design of potent PPARalpha agonists.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 17, Issue:11, 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
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
Structure-activity relationships of dimeric PPAR agonists.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 15, Issue:5, 2005
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
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
[no title available]Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
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
Phenoxy herbicides and fibrates potently inhibit the human chemosensory receptor subunit T1R3.Journal of medicinal chemistry, , Nov-12, Volume: 52, Issue:21, 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
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
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
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
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
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
Development of a new class of benzoylpyrrole-based PPARα/γ activators.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
Synthesis and pharmacological evaluation of novel benzoylazole-based PPAR α/γ activators.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 21, Issue:7, 2011
Ursolic acid is a PPAR-α agonist that regulates hepatic lipid metabolism.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 21, Issue:19, 2011
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
Identification and synthesis of a novel selective partial PPARdelta agonist with full efficacy on lipid metabolism in vitro and in vivo.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
Diphenylmethane skeleton as a multi-template for nuclear receptor ligands: preparation of FXR and PPAR ligands.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 16, Issue:12, 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
Tetrahydroisoquinoline PPARgamma agonists: design of novel, highly selective non-TZD antihyperglycemic agents.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 16, Issue:24, 2006
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
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
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
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
O-arylmandelic acids as highly selective human PPAR alpha/gamma agonists.Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 13, Issue:19, 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
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
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
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
Design, synthesis, and biological evaluation of novel thiazolidinediones as PPARγ/FFAR1 dual agonists.European journal of medicinal chemistry, , Feb-15, Volume: 109, 2016
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
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
Biological evaluation of novel benzisoxazole derivatives as PPARδ agonists.Bioorganic & medicinal chemistry, , May-15, Volume: 19, Issue:10, 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
(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
Acidic elements in histamine H(3) receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, Issue:5, 2010
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
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
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
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
Selective, potent PPARgamma agonists with cyclopentenone core structure.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 19, Issue:7, 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
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
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
Discovery of azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 18, Issue:6, 2008
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
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
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
Novel selective PPARdelta agonists: optimization of activity by modification of alkynylallylic moiety.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 17, Issue:15, 2007
Identification and synthesis of a novel selective partial PPARdelta agonist with full efficacy on lipid metabolism in vitro and in vivo.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
Design of a partial PPARdelta agonist.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 17, Issue:16, 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 of potent PPARalpha agonists.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 17, Issue:11, 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
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
Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 16, Issue:23, 2006
Tetrahydroisoquinoline PPARgamma agonists: design of novel, highly selective non-TZD antihyperglycemic agents.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 16, Issue:24, 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
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
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
Structure-activity relationships of dimeric PPAR agonists.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 15, Issue:5, 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
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
(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
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
5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.Bioorganic & medicinal chemistry letters, , May-19, Volume: 13, Issue:10, 2003
Amphipathic 3-phenyl-7-propylbenzisoxazoles; human pPaR gamma, delta and alpha agonists.Bioorganic & medicinal chemistry letters, , Mar-10, Volume: 13, Issue:5, 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
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 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
Phenylacetic acid derivatives as hPPAR agonists.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 13, Issue:7, 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
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
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 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
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
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. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents.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
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
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
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
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
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
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
Identification of the first potent, selective and bioavailable PPARα antagonist.Bioorganic & medicinal chemistry letters, , May-15, Volume: 24, Issue:10, 2014
(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
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 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
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
Phenolic Lipids Derived from Cashew Nut Shell Liquid to Treat Metabolic Diseases.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Discovery of (Journal of medicinal chemistry, , 07-28, Volume: 65, Issue:14, 2022
[no title available]Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Discovery of Pan-peroxisome Proliferator-Activated Receptor Modulators from an Endolichenic Fungus, Journal of natural products, , 12-23, Volume: 85, Issue:12, 2022
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
Design, Synthesis, and Biological Activity of l-1'-Homologated Adenosine Derivatives.ACS medicinal chemistry letters, , Jul-14, Volume: 13, Issue:7, 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
[no title available]Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
2-Phenyl-8-(1-phenylallyl)-chromenone compounds have a pan-PPAR modulator pharmacophore.Bioorganic & medicinal chemistry, , 07-01, Volume: 27, Issue:13, 2019
Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool.MedChemComm, , Aug-01, Volume: 10, Issue:8, 2019
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
Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.European journal of medicinal chemistry, , Nov-05, Volume: 159, 2018
Polypharmacology of NJournal of medicinal chemistry, , 09-14, Volume: 60, 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
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
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 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
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
Biological evaluation and structural insights for design of subtype-selective peroxisome proliferator activated receptor-α (PPAR-α) agonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 25, Issue:2, 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
trans-Caryophyllene is a natural agonistic ligand for peroxisome proliferator-activated receptor-α.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 24, Issue:14, 2014
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
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
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
Structural characterization of amorfrutins bound to the peroxisome proliferator-activated receptor γ.Journal of medicinal chemistry, , Feb-28, Volume: 56, Issue:4, 2013
Synthesis, radiolabeling and initial in vivo evaluation of [(11)C]KSM-01 for imaging PPAR-α receptors.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 22, Issue:19, 2012
Fibrate-derived N-(methylsulfonyl)amides with antagonistic properties on PPARα.European journal of medicinal chemistry, , Volume: 58, 2012
Targeting peroxisome proliferator-activated receptors (PPARs): development of modulators.Journal of medicinal chemistry, , May-10, Volume: 55, Issue:9, 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
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
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
Discovery of gemfibrozil analogues that activate PPARα and enhance the expression of gene CPT1A involved in fatty acids catabolism.European journal of medicinal chemistry, , Volume: 46, Issue:10, 2011
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
Benzothiazole-based N-(phenylsulfonyl)amides as a novel family of PPARα antagonists.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 21, Issue:16, 2011
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
Synthesis and biological evaluation of 2-heteroarylthioalkanoic acid analogues of clofibric acid as peroxisome proliferator-activated receptor alpha agonists.Journal of medicinal chemistry, , Oct-22, Volume: 52, Issue:20, 2009
Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
[no title available],
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
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
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
Discovery of Potent Dual PPARα Agonists/CB1 Ligands.ACS medicinal chemistry letters, , Nov-10, Volume: 2, Issue:11, 2011
Novel sulfamide analogs of oleoylethanolamide showing in vivo satiety inducing actions and PPARalpha activation.Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
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
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
[no title available],
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 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
Biological evaluation of novel benzisoxazole derivatives as PPARδ agonists.Bioorganic & medicinal chemistry, , May-15, Volume: 19, Issue:10, 2011
Phenoxyacetic acids as PPARδ partial agonists: synthesis, optimization, and in vivo efficacy.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 21, Issue:8, 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, molecular modeling studies and biological evaluation of fluorine substituted analogs of GW 501516.Bioorganic & medicinal chemistry, , Dec-01, Volume: 19, Issue:23, 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
Synthesis and SAR of selective benzothiophene, benzofuran, and indole-based peroxisome proliferator-activated receptor delta agonists.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 17, Issue:13, 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
Novel selective PPARdelta agonists: optimization of activity by modification of alkynylallylic moiety.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 17, Issue:15, 2007
Identification and synthesis of a novel selective partial PPARdelta agonist with full efficacy on lipid metabolism in vitro and in vivo.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 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
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
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
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
[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
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 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
Targeting peroxisome proliferator-activated receptors (PPARs): development of modulators.Journal of medicinal chemistry, , May-10, Volume: 55, Issue:9, 2012
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
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
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
Activity landscape modeling of PPAR ligands with dual-activity difference maps.Bioorganic & medicinal chemistry, , Jun-01, Volume: 20, Issue:11, 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
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
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
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
[no title available],
Activity landscape modeling of PPAR ligands with dual-activity difference maps.Bioorganic & medicinal chemistry, , Jun-01, Volume: 20, Issue:11, 2012
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
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
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
Targeting peroxisome proliferator-activated receptors (PPARs): development of modulators.Journal of medicinal chemistry, , May-10, Volume: 55, Issue:9, 2012
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
Biological evaluation of novel benzisoxazole derivatives as PPARδ agonists.Bioorganic & medicinal chemistry, , May-15, Volume: 19, Issue:10, 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
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
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
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
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
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
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
Discovery of potent and selective PPARα/δ dual antagonists and initial biological studies.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 29, Issue:3, 2019
Identification of the first potent, selective and bioavailable PPARα antagonist.Bioorganic & medicinal chemistry letters, , May-15, Volume: 24, Issue:10, 2014
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 23 target(s):
Target | Category | Definition |
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] |
DNA-binding transcription activator activity | molecular function | A DNA-binding transcription factor activity that activates or increases transcription of specific gene sets. [GOC:txnOH-2018] |
transcription coactivator binding | molecular function | Binding to a transcription coactivator, a protein involved in positive regulation of transcription via protein-protein interactions with transcription factors and other proteins that positively regulate transcription. Transcription coactivators do not bind DNA directly, but rather mediate protein-protein interactions between activating transcription factors and the basal transcription machinery. [GOC:krc] |
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] |
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] |
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] |
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 steroid receptor activity | molecular function | Combining with a steroid hormone and transmitting the signal within the cell to initiate a change in cell activity or function. [GOC:signaling, PMID:14708019] |
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] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
lipid binding | molecular function | Binding to a lipid. [GOC:ai] |
phosphatase binding | molecular function | Binding to a phosphatase. [GOC:jl] |
protein domain specific binding | molecular function | Binding to a specific domain of a protein. [GOC:go_curators] |
mitogen-activated protein kinase kinase kinase binding | molecular function | Binding to a mitogen-activated protein kinase kinase kinase, a protein that can phosphorylate a MAP kinase kinase. [GOC:bf] |
ubiquitin conjugating enzyme binding | molecular function | Binding to a ubiquitin conjugating enzyme, any of the E2 proteins. [GOC:vp] |
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] |
protein-containing complex binding | molecular function | Binding to a macromolecular complex. [GOC:jl] |
NFAT protein binding | molecular function | Binding to NFAT (nuclear factor of activated T cells) proteins, a family of transcription factors. NFAT proteins have crucial roles in the development and function of the immune system. [PMID:15928679] |
RNA polymerase II-specific DNA-binding transcription factor binding | molecular function | Binding to a sequence-specific DNA binding RNA polymerase II transcription factor, any of the factors that interact selectively and non-covalently with a specific DNA sequence in order to modulate transcription. [GOC:dph, GOC:vw] |
MDM2/MDM4 family protein binding | molecular function | Binding to a member of the MDM2/MDM4 protein family, comprising negative regulators of p53. [InterPro:IPR016495] |
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] |
Located In
This protein is located in 2 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] |
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 1 target(s):
Target | Category | Definition |
chromatin | cellular component | The ordered and organized complex of DNA, protein, and sometimes RNA, that forms the chromosome. [GOC:elh, PMID:20404130] |
Involved In
This protein is involved in 42 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] |
response to hypoxia | 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 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:hjd] |
gluconeogenesis | biological process | The formation of glucose from noncarbohydrate precursors, such as pyruvate, amino acids and glycerol. [MetaCyc:GLUCONEO-PWY] |
heart development | biological process | The process whose specific outcome is the progression of the heart over time, from its formation to the mature structure. The heart is a hollow, muscular organ, which, by contracting rhythmically, keeps up the circulation of the blood. [GOC:jid, UBERON:0000948] |
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] |
epidermis development | biological process | The process whose specific outcome is the progression of the epidermis over time, from its formation to the mature structure. The epidermis is the outer epithelial layer of an animal, it may be a single layer that produces an extracellular material (e.g. the cuticle of arthropods) or a complex stratified squamous epithelium, as in the case of many vertebrate species. [GOC:go_curators, UBERON:0001003] |
cellular response to starvation | 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 deprivation of nourishment. [GOC:jl] |
regulation of cellular ketone metabolic process | biological process | Any process that modulates the chemical reactions and pathways involving any of a class of organic compounds that contain the carbonyl group, CO, and in which the carbonyl group is bonded only to carbon atoms. The general formula for a ketone is RCOR, where R and R are alkyl or aryl groups. [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 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] |
regulation of fatty acid metabolic process | biological process | Any process that modulates the frequency, rate or extent of the chemical reactions and pathways involving fatty acids. [GOC:go_curators] |
intracellular receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to a receptor located within a cell. [GOC:bf, GOC:mah] |
positive regulation of fatty acid beta-oxidation | biological process | Any process that activates or increases the frequency, rate or extent of fatty acid beta-oxidation. [GOC:mah] |
negative regulation of appetite | biological process | Any process that reduces appetite. [GOC:add] |
response to insulin | 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 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] |
circadian regulation of gene expression | biological process | Any process that modulates the frequency, rate or extent of gene expression such that an expression pattern recurs with a regularity of approximately 24 hours. [GOC:mah] |
behavioral response to nicotine | biological process | Any process that results in a change in the behavior of an organism as a result of a nicotine stimulus. [GOC:bf, ISBN:0198506732] |
wound healing | biological process | The series of events that restore integrity to a damaged tissue, following an injury. [GOC:bf, PMID:15269788] |
lipoprotein metabolic process | biological process | The chemical reactions and pathways involving any conjugated, water-soluble protein in which the covalently attached nonprotein group consists of a lipid or lipids. [ISBN:0198506732] |
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] |
steroid hormone mediated signaling pathway | biological process | The series of molecular signals mediated by a steroid hormone binding to a receptor. [PMID:12606724] |
response to ethanol | 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 an ethanol stimulus. [GOC:go_curators] |
positive regulation of gluconeogenesis | biological process | Any process that activates or increases the frequency, rate or extent of gluconeogenesis. [GOC:go_curators] |
negative regulation of blood pressure | biological process | Any process in which the force of blood traveling through the circulatory system is decreased. [GOC:go_curators, GOC:mtg_cardio] |
negative regulation of glycolytic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of glycolysis. [GOC:go_curators] |
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] |
nitric oxide metabolic process | biological process | The chemical reactions and pathways involving nitric oxide, nitrogen monoxide (NO), a colorless gas only slightly soluble in water. [GOC:ai] |
positive regulation of fatty acid oxidation | biological process | Any process that activates or increases the frequency, rate or extent of fatty acid oxidation. [GOC:ai] |
positive regulation of lipid biosynthetic process | biological process | Any process that activates or increases the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of lipids. [GOC:ai] |
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] |
negative regulation of cell growth involved in cardiac muscle cell development | biological process | Any process that decreases the rate, frequency, or extent of the growth of a cardiac muscle cell, where growth contributes to the progression of the cell over time from its initial formation to its mature state. [GOC:dph] |
enamel mineralization | biological process | The process in which calcium salts, mainly carbonated hydroxyapatite, are deposited in tooth enamel. [GOC:BHF, GOC:mah, GOC:sl, PMID:10206335, PMID:16931858, PMID:21196346] |
cellular response to fructose 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 fructose stimulus. [GOC:mah] |
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] |
negative regulation of leukocyte cell-cell adhesion | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of leukocyte cell-cell adhesion. [GO_REF:0000058, GOC:BHF, GOC:rl, GOC:TermGenie, PMID:21106532] |
regulation of fatty acid transport | biological process | Any process that modulates the frequency, rate or extent of fatty acid transport. [GOC:BHF] |
hormone-mediated signaling pathway | biological process | The series of molecular signals mediated by the detection of a hormone. [GOC:sm] |
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] |
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] |
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] |