Proteins > Peroxisome proliferator-activated receptor delta
Page last updated: 2024-08-07 17:00:08
Peroxisome proliferator-activated receptor delta
A peroxisome proliferator-activated receptor delta that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q03181]
Synonyms
PPAR-delta;
NUCI;
Nuclear hormone receptor 1;
NUC1;
Nuclear receptor subfamily 1 group C member 2;
Peroxisome proliferator-activated receptor beta;
PPAR-beta
Research
Bioassay Publications (106)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 2 (1.89) | 18.2507 |
2000's | 40 (37.74) | 29.6817 |
2010's | 47 (44.34) | 24.3611 |
2020's | 17 (16.04) | 2.80 |
Compounds (45)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
myristic acid | Homo sapiens (human) | Emax | 51.0000 | 1 | 1 |
anacardic acid | Homo sapiens (human) | Emax | 68.0000 | 1 | 1 |
farglitazar | Homo sapiens (human) | Log Ki | 6.0700 | 1 | 1 |
oleic acid | Homo sapiens (human) | Emax | 47.0000 | 1 | 1 |
gw 1929 | Homo sapiens (human) | Log Ki | 6.1500 | 1 | 1 |
Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation.Journal of medicinal chemistry, , 02-28, Volume: 62, Issue:4, 2019
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
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
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
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
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
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
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, molecular modeling studies and biological evaluation of fluorine substituted analogs of GW 501516.Bioorganic & medicinal chemistry, , Dec-01, Volume: 19, Issue:23, 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
Biological evaluation of novel benzisoxazole derivatives as PPARδ agonists.Bioorganic & medicinal chemistry, , May-15, Volume: 19, Issue:10, 2011
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
Selective, potent PPARgamma agonists with cyclopentenone core structure.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 19, Issue:7, 2009
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, 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
(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
5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.Bioorganic & medicinal chemistry letters, , May-19, Volume: 13, Issue:10, 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
Phenylacetic acid derivatives as hPPAR agonists.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 13, Issue:7, 2003
Amphipathic 3-phenyl-7-propylbenzisoxazoles; human pPaR gamma, delta and alpha agonists.Bioorganic & medicinal chemistry letters, , Mar-10, Volume: 13, Issue:5, 2003
Biological evaluation of novel benzisoxazole derivatives as PPARδ agonists.Bioorganic & medicinal chemistry, , May-15, Volume: 19, Issue:10, 2011
The PPARs: from orphan receptors to drug discovery.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
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
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
Synthesis of 5-trifluoromethyl-2-sulfonylpyridine PPARβ/δ antagonists: Effects on the affinity and selectivity towards PPARβ/δ.Bioorganic & medicinal chemistry, , Jan-15, Volume: 24, Issue:2, 2016
Synthesis, biological evaluation and molecular modeling studies of the PPARβ/δ antagonist CC618.European journal of medicinal chemistry, , Apr-13, Volume: 94, 2015
Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
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
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
Discovery of (Journal of medicinal chemistry, , 07-28, Volume: 65, Issue:14, 2022
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
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
Synthesis and evaluation of 4-cycloheptylphenols as selective Estrogen receptor-β agonists (SERBAs).European journal of medicinal chemistry, , Sep-05, Volume: 157, 2018
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
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
Structural development studies of PPARs ligands based on tyrosine scaffold.European journal of medicinal chemistry, , Jan-07, Volume: 89, 2015
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
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
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
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
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
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
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 Activity of l-1'-Homologated Adenosine Derivatives.ACS medicinal chemistry letters, , Jul-14, Volume: 13, Issue:7, 2022
[no title available]Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
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
Targeting Peroxisome Proliferator-Activated Receptor Delta (PPARδ): A Medicinal Chemistry Perspective.Journal of medicinal chemistry, , 09-24, Volume: 63, Issue:18, 2020
[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
2-Phenyl-8-(1-phenylallyl)-chromenone compounds have a pan-PPAR modulator pharmacophore.Bioorganic & medicinal chemistry, , 07-01, Volume: 27, Issue:13, 2019
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
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
Polypharmacology of NJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 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 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
Synthesis, biological evaluation and molecular modeling studies of the PPARβ/δ antagonist CC618.European journal of medicinal chemistry, , Apr-13, Volume: 94, 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
Activity landscape modeling of PPAR ligands with dual-activity difference maps.Bioorganic & medicinal chemistry, , Jun-01, Volume: 20, Issue:11, 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, 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
Discovery of isoindoline and tetrahydroisoquinoline derivatives as potent, selective PPARδ agonists.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 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
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
Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Novel bisaryl substituted thiazoles and oxazoles as highly potent and selective peroxisome proliferator-activated receptor delta agonists.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
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
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, 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
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 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
Phenylpropanoic acid derivatives bearing a benzothiazole ring as PPARdelta-selective agonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 17, Issue:15, 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
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
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 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
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
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
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
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
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
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
Phenolic Lipids Derived from Cashew Nut Shell Liquid to Treat Metabolic Diseases.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 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
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
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
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
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 first-in-class thiazole-based dual FFA1/PPARδ agonists as potential anti-diabetic agents.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
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
Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.European journal of medicinal chemistry, , Nov-05, Volume: 159, 2018
Syringaresinol induces mitochondrial biogenesis through activation of PPARβ pathway in skeletal muscle cells.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 26, Issue:16, 2016
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
Structural characterization of amorfrutins bound to the peroxisome proliferator-activated receptor γ.Journal of medicinal chemistry, , Feb-28, Volume: 56, Issue:4, 2013
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
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
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, 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
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
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
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
The discovery of equipotent PPARalpha/gamma dual activators.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 18, Issue:23, 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
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
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
Design, Synthesis, and Biological Activity of l-1'-Homologated Adenosine Derivatives.ACS medicinal chemistry letters, , Jul-14, Volume: 13, Issue:7, 2022
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
[no title available]Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Synthesis, biological evaluation and molecular modeling studies of the PPARβ/δ antagonist CC618.European journal of medicinal chemistry, , Apr-13, Volume: 94, 2015
Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
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 14 target(s):
Target | Category | Definition |
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 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 | 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] |
linoleic acid binding | molecular function | Binding to linoleic acid, the 18-carbon unsaturated fatty acid (9Z,12Z)-octadeca-9,12-dienoic acid. [GOC:lp, GOC:mah] |
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] |
sequence-specific double-stranded DNA binding | molecular function | Binding to double-stranded 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:dos, GOC:sl] |
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] |
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 47 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] |
glucose metabolic process | biological process | The chemical reactions and pathways involving glucose, the aldohexose gluco-hexose. D-glucose is dextrorotatory and is sometimes known as dextrose; it is an important source of energy for living organisms and is found free as well as combined in homo- and hetero-oligosaccharides and polysaccharides. [ISBN:0198506732] |
generation of precursor metabolites and energy | biological process | The chemical reactions and pathways resulting in the formation of precursor metabolites, substances from which energy is derived, and any process involved in the liberation of energy from these substances. [GOC:jl] |
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] |
fatty acid beta-oxidation | biological process | A fatty acid oxidation process that results in the complete oxidation of a long-chain fatty acid. Fatty acid beta-oxidation begins with the addition of coenzyme A to a fatty acid, and occurs by successive cycles of reactions during each of which the fatty acid is shortened by a two-carbon fragment removed as acetyl coenzyme A; the cycle continues until only two or three carbons remain (as acetyl-CoA or propionyl-CoA respectively). [GOC:mah, ISBN:0198506732, MetaCyc:FAO-PWY] |
apoptotic process | biological process | A programmed cell death process which begins when a cell receives an internal (e.g. DNA damage) or external signal (e.g. an extracellular death ligand), and proceeds through a series of biochemical events (signaling pathway phase) which trigger an execution phase. The execution phase is the last step of an apoptotic process, and is typically characterized by rounding-up of the cell, retraction of pseudopodes, reduction of cellular volume (pyknosis), chromatin condensation, nuclear fragmentation (karyorrhexis), plasma membrane blebbing and fragmentation of the cell into apoptotic bodies. When the execution phase is completed, the cell has died. [GOC:cjm, GOC:dhl, GOC:ecd, GOC:go_curators, GOC:mtg_apoptosis, GOC:tb, ISBN:0198506732, PMID:18846107, PMID:21494263] |
embryo implantation | biological process | Attachment of the blastocyst to the uterine lining. [GOC:isa_complete, http://www.medterms.com] |
cholesterol metabolic process | biological process | The chemical reactions and pathways involving cholesterol, cholest-5-en-3 beta-ol, the principal sterol of vertebrates and the precursor of many steroids, including bile acids and steroid hormones. It is a component of the plasma membrane lipid bilayer and of plasma lipoproteins and can be found in all animal tissues. [ISBN:0198506732] |
cell population proliferation | biological process | The multiplication or reproduction of cells, resulting in the expansion of a cell population. [GOC:mah, GOC:mb] |
axon ensheathment | biological process | Any process in which the axon of a neuron is insulated, and that insulation maintained, thereby preventing dispersion of the electrical signal. [GOC:jl, ISBN:0878932437] |
fatty acid catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of a fatty acid, any of the aliphatic monocarboxylic acids that can be liberated by hydrolysis from naturally occurring fats and oils. Fatty acids are predominantly straight-chain acids of 4 to 24 carbon atoms, which may be saturated or unsaturated; branched fatty acids and hydroxy fatty acids also occur, and very long chain acids of over 30 carbons are found in waxes. [GOC:go_curators] |
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] |
regulation of skeletal muscle satellite cell proliferation | biological process | Any process that modulates the frequency, rate or extent of skeletal muscle satellite cell proliferation. [GOC:ef, GOC:mtg_muscle, PMID:16607119] |
fatty acid transport | biological process | The directed movement of fatty acids into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Fatty acids are aliphatic monocarboxylic acids liberated from naturally occurring fats and oils by hydrolysis. [GOC:ai] |
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] |
cell-substrate adhesion | biological process | The attachment of a cell to the underlying substrate via adhesion molecules. [GOC:mah, GOC:pf] |
cellular response to nutrient levels | 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 reflecting the presence, absence, or concentration of nutrients. [GOC:mah] |
wound healing | biological process | The series of events that restore integrity to a damaged tissue, following an injury. [GOC:bf, PMID:15269788] |
steroid hormone mediated signaling pathway | biological process | The series of molecular signals mediated by a steroid hormone binding to a receptor. [PMID:12606724] |
positive regulation of skeletal muscle tissue regeneration | biological process | Any process that activates or increase the rate of skeletal muscle regeneration. [GOC:jl] |
phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | An intracellular signaling cassette that starts with phosphatidylinositol 3-kinase (PI3K) activation, production of phosphatidylinositol 3-phosphate (PI3P), activation of PDK1, which recruits and ending with the activation of protein kinase B (PKB, also known as Akt). PI3K is activated by cell surface receptors. Note that PTEN is an inhibitor of the pathway. [PMID:20517722, PMID:22952397] |
keratinocyte proliferation | biological process | The multiplication or reproduction of keratinocytes, resulting in the expansion of a cell population. Keratinocytes are epidermal cells which synthesize keratin and undergo a characteristic change as they move upward from the basal layers of the epidermis to the cornified (horny) layer of the skin. [CL:0000311] |
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 myoblast differentiation | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of myoblast differentiation. A myoblast is a mononucleate cell type that, by fusion with other myoblasts, gives rise to the myotubes that eventually develop into skeletal muscle fibers. [CL:0000056, GOC:go_curators, GOC:mtg_muscle] |
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] |
decidualization | biological process | The cellular and vascular changes occurring in the endometrium of the pregnant uterus just after the onset of blastocyst implantation. This process involves the proliferation and differentiation of the fibroblast-like endometrial stromal cells into large, polyploid decidual cells that eventually form the maternal component of the placenta. [ISBN:0721662544, PMID:11133685] |
negative regulation of epithelial cell proliferation | biological process | Any process that stops, prevents or reduces the rate or extent of epithelial cell proliferation. [GOC:ai] |
keratinocyte migration | biological process | The directed movement of a keratinocyte, epidermal cells which synthesize keratin, from one site to another. [ISBN:0721662544] |
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of phosphatidylinositol 3-kinase/protein kinase B signal transduction. [GOC:ai] |
adipose tissue development | biological process | The process whose specific outcome is the progression of adipose tissue over time, from its formation to the mature structure. Adipose tissue is specialized tissue that is used to store fat. [GOC:dph] |
fat cell proliferation | biological process | The multiplication or reproduction of fat cells by cell division, resulting in the expansion of their population. A fat cell is an animal connective tissue cell specialized for the synthesis and storage of fat. [GOC:mah, GOC:sl] |
positive regulation of fat cell proliferation | biological process | Any process that activates or increases the rate or extent of fat cell proliferation. [GOC:mah, GOC:sl] |
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] |
energy homeostasis | biological process | Any process involved in the balance between food intake (energy input) and energy expenditure. [GOC:yaf, PMID:15919751] |
apoptotic signaling pathway | biological process | The series of molecular signals which triggers the apoptotic death of a cell. The pathway starts with reception of a signal, and ends when the execution phase of apoptosis is triggered. [GOC:mtg_apoptosis] |
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] |
glucose transmembrane transport | biological process | The process in which glucose is transported across a membrane. [GO_REF:0000069, GOC:TermGenie, PMID:9090050] |
positive regulation of myoblast proliferation | biological process | Any process that activates or increases the frequency, rate or extent of myoblast proliferation. [GOC:BHF] |
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] |
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] |
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 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] |
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] |
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] |
hormone-mediated signaling pathway | biological process | The series of molecular signals mediated by the detection of a hormone. [GOC:sm] |