Target Information

Target General Infomation
Target ID
T86591
Former ID
TTDS00340
Target Name
Peroxisome proliferator activated receptor alpha
Gene Name
PPARA
Synonyms
PPAR-alpha; PPARalpha; Peroxisome proliferater-activated receptor alpha; PPARA
Target Type
Successful
Disease Arteriosclerosis [ICD9: 440; ICD10: I70]
Cardiovascular disorder [ICD10: I00-I99]
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1]
Dyslipidaemias [ICD9: 272; ICD10: E78]
Gout [ICD9: 274.00274.1274.8274.9; ICD10: M10]
Hyperlipidaemia [ICD9: 272.0-272.4; ICD10: E78]
Hyperlipoproteinemia; Atherosclerosis [ICD9:272.0-272.4, 414.0, 440; ICD10: E78, I70]
Heart failure [ICD9: 428; ICD10: I50]
High cholesterol level; High triglyceride level [ICD9: 272.0, 272.1; ICD10: E78.0, E78.1, E78.2, E78.3]
Lipid metabolism disorder [ICD10: E75-E78]
Metabolic disorders [ICD9: 270-279; ICD10: E70-E89]
Non-alcoholic fatty liver disease [ICD9: 571.8; ICD10: K76.0]
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06]
Type 2 diabetes [ICD9: 250; ICD10: E11]
Type 1 diabetes [ICD9: 250; ICD10: E10]
Unspecified [ICD code not available]
Function
Ligand-activated transcription factor. Key regulator of lipid metabolism. Activated by the endogenous ligand 1-palmitoyl- 2-oleoyl-sn-glycerol-3-phosphocholine (16:0/18:1-GPC). Activated by oleylethanolamide, a naturally occurring lipid that regulates satiety. Receptor for peroxisome proliferators such as hypolipidemic drugs and fatty acids. Regulates the peroxisomal beta-oxidation pathway of fatty acids. Functions as transcription activator for the ACOX1 and P450 genes. Transactivation activity requires heterodimerization with RXRA and is antagonized by NR2C2. May be required for the propagation of clock information to metabolic pathways regulated by PER2.
BioChemical Class
Zinc-finger
Target Validation
T86591
UniProt ID
Q07869
Sequence
MVDTESPLCPLSPLEAGDLESPLSEEFLQEMGNIQEISQSIGEDSSGSFGFTEYQYLGSC
PGSDGSVITDTLSPASSPSSVTYPVVPGSVDESPSGALNIECRICGDKASGYHYGVHACE
GCKGFFRRTIRLKLVYDKCDRSCKIQKKNRNKCQYCRFHKCLSVGMSHNAIRFGRMPRSE
KAKLKAEILTCEHDIEDSETADLKSLAKRIYEAYLKNFNMNKVKARVILSGKASNNPPFV
IHDMETLCMAEKTLVAKLVANGIQNKEAEVRIFHCCQCTSVETVTELTEFAKAIPGFANL
DLNDQVTLLKYGVYEAIFAMLSSVMNKDGMLVAYGNGFITREFLKSLRKPFCDIMEPKFD
FAMKFNALELDDSDISLFVAAIICCGDRPGLLNVGHIEKMQEGIVHVLRLHLQSNHPDDI
FLFPKLLQKMADLRQLVTEHAQLVQIIKKTESDAALHPLLQEIYRDMY
Drugs and Mode of Action
Drug(s) Bezafibrate Drug Info Approved Hyperlipidaemia [539733], [550550]
Ciprofibrate Drug Info Approved Hyperlipoproteinemia; Atherosclerosis [540377], [550550], [551871]
Fenofibrate Drug Info Approved High cholesterol level; High triglyceride level [536740], [542197]
CS-038 Drug Info Phase 3 Type 2 diabetes [524807]
Imiglitazar Drug Info Phase 3 Type 2 diabetes [525383], [539741]
K-877 Drug Info Phase 3 Lipid metabolism disorder [549140]
Lobeglitazone Drug Info Phase 3 Diabetes [531686]
MURAGLITAZAR Drug Info Phase 3 Discovery agent [521615]
Ragaglitazar Drug Info Phase 3 Type 1 diabetes [526845], [539729]
TESAGLITAZAR Drug Info Phase 3 Type 1 diabetes [521734]
ZYH-1 Drug Info Phase 3 Lipid metabolism disorder [532516]
GFT-505 Drug Info Phase 2 Type 2 diabetes [548380]
GFT14 Drug Info Phase 2 Hyperlipidaemia [548300]
LY-518674 Drug Info Phase 2 Diabetes [521832], [539724]
Naveglitazar Drug Info Phase 2 Diabetes [521566]
ONO-5129 Drug Info Phase 2 Diabetes [521841]
ZYH-7 Drug Info Phase 2 Lipid metabolism disorder [523803]
AVE0897 Drug Info Phase 1 Type 2 diabetes [548128]
CDT-fenofibrate Drug Info Phase 1 Hyperlipidaemia [534742]
GW-409544 Drug Info Phase 1 Hyperlipidaemia [531939], [540380]
Oxeglitazar Drug Info Phase 1 Gout [531047]
MC-3001 Drug Info Preclinical Lipid metabolism disorder [548011]
MC-3002 Drug Info Preclinical Metabolic disorders [548000]
Romazarit Drug Info Preclinical Rheumatoid arthritis [544776]
Aleglitazar Drug Info Discontinued in Phase 3 Type 2 diabetes [542428], [547561]
AVE-0847 Drug Info Discontinued in Phase 2 Hyperlipidaemia [547944]
AVE-8134 Drug Info Discontinued in Phase 2 Heart failure [548007]
BM-17.0744 Drug Info Discontinued in Phase 2 Type 1 diabetes [546978]
GSK-677954 Drug Info Discontinued in Phase 2 Non-alcoholic fatty liver disease [536649]
Indeglitazar Drug Info Discontinued in Phase 2 Type 2 diabetes [548153]
KRP-101 Drug Info Discontinued in Phase 2 Hyperlipidaemia [547707]
MK-767 (KRP-297) Drug Info Discontinued in Phase 2 Type 2 diabetes [546825]
NS-220 Drug Info Discontinued in Phase 2 Hyperlipidaemia [539744], [547609]
Reglixane Drug Info Discontinued in Phase 2 Diabetes [546560]
Sodelglitazar Drug Info Discontinued in Phase 2 Hyperlipidaemia [547644]
AR-H049020 Drug Info Discontinued in Phase 1 Type 1 diabetes [547411]
DRF 10945 Drug Info Discontinued in Phase 1 Hyperlipidaemia [547933]
E-3030 Drug Info Discontinued in Phase 1 Hyperlipidaemia [548044]
LG-101280 Drug Info Discontinued in Phase 1 Arteriosclerosis [547284]
LY-929 Drug Info Discontinued in Phase 1 Lipid metabolism disorder [539723], [547284]
MP-136 Drug Info Discontinued in Phase 1 Lipid metabolism disorder [548975]
BVT-142 Drug Info Terminated Type 2 diabetes [527135]
CS-204 Drug Info Terminated Metabolic disorders [548591]
CS-207 Drug Info Terminated Cardiovascular disorder [548592]
KRP-105 Drug Info Terminated Lipid metabolism disorder [548566]
KRP-297 Drug Info Terminated Hyperlipidaemia [526192], [539743]
Sipoglitazar Drug Info Terminated Diabetes [532486]
Inhibitor (9Z,12E)-12-nitrooctadeca-9,12-dienoic acid Drug Info [530350]
(E)-12-Nitrooctadec-12-enoic Acid Drug Info [530350]
(E)-13-Nitrooctadec-12-enoic Acid Drug Info [530350]
BMS-687453 Drug Info [530777]
Deoxy-Bigchap Drug Info [551393]
GSK-9578 Drug Info [526879]
L-165461 Drug Info [526582]
L-796449 Drug Info [526582]
PIRINIXIC ACID Drug Info [526707]
Agonist 8S-HETE Drug Info [533647]
AD-5061 Drug Info [527124]
Aleglitazar Drug Info [551607]
AR-H049020 Drug Info [550118]
AVE-8134 Drug Info [530192]
AVE0897 Drug Info [549823]
Bezafibrate Drug Info [537006]
BVT-142 Drug Info [527135], [550926]
CDT-fenofibrate Drug Info [534742]
Ciprofibrate Drug Info [534997]
CP-775146 Drug Info [529780]
CS-204 Drug Info [544056]
CS-207 Drug Info [548593]
DB-900 Drug Info [550862]
DRF 10945 Drug Info [544209]
DRF 2519 Drug Info [527076]
eicosatetranoic acid Drug Info [534452]
Fenofibrate Drug Info [534997]
Fibrates Drug Info [536740]
GFT14 Drug Info [548301]
GSK-677954 Drug Info [536649]
GW7647 Drug Info [526054]
GW9578 Drug Info [534997]
Indeglitazar Drug Info [529893]
K-877 Drug Info [532380]
KRP-101 Drug Info [529268], [530129]
KRP-105 Drug Info [531722]
Lobeglitazone Drug Info [531686]
LY-465608 Drug Info [527060]
LY-518674 Drug Info [529793]
LY-929 Drug Info [550832]
MC-3001 Drug Info [548012]
MP-136 Drug Info [543889]
N-oleoylethanolamide Drug Info [527561]
NS-220 Drug Info [529786], [551871]
pristanic acid Drug Info [525897]
pterostilbene Drug Info [543889]
reglitazar Drug Info [534829]
Sodelglitazar Drug Info [531487]
TZD18 Drug Info [526920]
Modulator AVE-0847 Drug Info
CS-038 Drug Info
E-3030 Drug Info
GFT-505 Drug Info
GW-2331 Drug Info
GW-409544 Drug Info [531939]
Imiglitazar Drug Info [527124]
KRP-297 Drug Info [526192]
LG-101280 Drug Info [527514]
LL-6531 Drug Info [543889]
MC-3002 Drug Info [1572591]
MK-767 (KRP-297) Drug Info [526645]
MURAGLITAZAR Drug Info
Naveglitazar Drug Info [528458]
ONO-5129 Drug Info [1572591]
Oxeglitazar Drug Info [531047]
Ragaglitazar Drug Info [526845]
Reglixane Drug Info [1572591]
Romazarit Drug Info [544293]
Sipoglitazar Drug Info [532486]
TESAGLITAZAR Drug Info
ZY H2 Drug Info [1572605]
ZYH-1 Drug Info [532486]
ZYH-7 Drug Info [543889]
Activator BM-17.0744 Drug Info [526404], [551871]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway PPAR signaling pathway
cAMP signaling pathway
Adipocytokine signaling pathway
Glucagon signaling pathway
Non-alcoholic fatty liver disease (NAFLD)
Hepatitis C
Pathway Interaction Database RXR and RAR heterodimerization with other nuclear receptor
Reactome RORA activates gene expression
CLOCK,NPAS2 activates circadian gene expression
PPARA activates gene expression
YAP1- and WWTR1 (TAZ)-stimulated gene expression
Transcriptional activation of mitochondrial biogenesis
Activation of gene expression by SREBF (SREBP)
Transcriptional regulation of white adipocyte differentiation
Nuclear Receptor transcription pathway
Regulation of lipid metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha)
Circadian Clock
WikiPathways Nuclear Receptors in Lipid Metabolism and Toxicity
Nuclear Receptors Meta-Pathway
Estrogen Receptor Pathway
PPAR Alpha Pathway
Regulation of Lipid Metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha)
Transcriptional Regulation of White Adipocyte Differentiation
YAP1- and WWTR1 (TAZ)-stimulated gene expression
Activation of Gene Expression by SREBP (SREBF)
Adipogenesis
SREBF and miR33 in cholesterol and lipid homeostasis
Circadian Clock
Nuclear Receptors
References
Ref 521566ClinicalTrials.gov (NCT00065312) An Evaluation of an Oral Antidiabetic Agent for the Treatment of Type 2 Diabetes. U.S. National Institutes of Health.
Ref 521615ClinicalTrials.gov (NCT00094991) Mechanism of Action and Efficacy of Muraglitazar in Type 2 Diabetes. U.S. National Institutes of Health.
Ref 521734ClinicalTrials.gov (NCT00229710) GALLEX 9: Safety and Tolerability of Oral Tesaglitazar When Added to Insulin Therapy in Patients With Type 2 Diabetes. U.S. National Institutes of Health.
Ref 521832ClinicalTrials.gov (NCT00327002) A Mechanistic Study of the Effects of LY518674 on High-Density Lipoprotein Cholesterol (HDL-C) Metabolism. U.S. National Institutes of Health.
Ref 521841ClinicalTrials.gov (NCT00335712) Pilot Study of ONO-5129 in Patients With Type 2 Diabetes Mellitus. U.S. National Institutes of Health.
Ref 523803ClinicalTrials.gov (NCT01539616) A Clinical Trial to Evaluate the Safety and Efficacy of ZYH7 Compared to Fenofibrate in Patients With Dyslipidemia. U.S. National Institutes of Health.
Ref 524807ClinicalTrials.gov (NCT02173457) Study of Chiglitazar Compare With Sitagliptin in Type 2 Diabetes Patients. U.S. National Institutes of Health.
Ref 525383Medicinal Chemistry and Actions of Dual and Pan PPAR Modulators. Open Med Chem J. 2011;5(Suppl 2):93-8.
Ref 526192KRP-297, MCC-555. Nihon Rinsho. 2001 Nov;59(11):2200-6.
Ref 526845Ragaglitazar: the pharmacokinetics, pharmacodynamics, and tolerability of a novel dual PPAR alpha and gamma agonist in healthy subjects and patients with type 2 diabetes. J Clin Pharmacol. 2003 Nov;43(11):1244-56.
Ref 527135A new class of peroxisome proliferator-activated receptor agonists with a novel binding epitope shows antidiabetic effects. J Biol Chem. 2004 Sep 24;279(39):41124-30. Epub 2004 Jul 15.
Ref 531047Therapeutic potential of aleglitazar, a new dual PPAR-alpha/gamma agonist: implications for cardiovascular disease in patients with diabetes mellitus. Am J Cardiovasc Drugs. 2010;10(4):209-16.
Ref 531686Tolerability and pharmacokinetics of lobeglitazone (CKD-501), a peroxisome proliferator-activated receptor-gamma agonist: a single- and multiple-dose, double-blind, randomized control study in healthy male Korean subjects. Clin Ther. 2011 Nov;33(11):1819-30.
Ref 531939Design novel dual agonists for treating type-2 diabetes by targeting peroxisome proliferator-activated receptors with core hopping approach. PLoS One. 2012;7(6):e38546.
Ref 532486Pharmacokinetics, safety, and tolerability of saroglitazar (ZYH1), a predominantly PPARalpha agonist with moderate PPARgamma agonist activity in healthy human subjects. Clin Drug Investig. 2013 Nov;33(11):809-16.
Ref 532516A multicenter, prospective, randomized, double-blind study to evaluate the safety and efficacy of Saroglitazar 2 and 4??g compared with placebo in type 2 diabetes mellitus patients having hypertriglyceridemia not controlled with atorvastatin therapy (PRESS VI). Diabetes Technol Ther. 2014 Feb;16(2):63-71.
Ref 534742Mechanism of action of fibrates on lipid and lipoprotein metabolism. Circulation. 1998 Nov 10;98(19):2088-93.
Ref 536649Emerging drugs for non-alcoholic fatty liver disease. Expert Opin Emerg Drugs. 2008 Mar;13(1):145-58.
Ref 536740Emerging antidyslipidemic drugs. Expert Opin Emerg Drugs. 2008 Jun;13(2):363-81.
Ref 539723(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2657).
Ref 539724(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2658).
Ref 539729(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2664).
Ref 539733(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2668).
Ref 539741(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2675).
Ref 539743(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2677).
Ref 539744(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2678).
Ref 540377(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3438).
Ref 540380(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3440).
Ref 542197(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7186).
Ref 542428(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7405).
Ref 544776Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000969)
Ref 546560Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008953)
Ref 546825Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010490)
Ref 546978Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011739)
Ref 547284Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014823)
Ref 547411Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016001)
Ref 547561Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017317)
Ref 547609Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017798)
Ref 547644Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018093)
Ref 547707Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018628)
Ref 547933Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020522)
Ref 547944Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020608)
Ref 548000Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021065)
Ref 548007Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021122)
Ref 548011Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021175)
Ref 548044Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021476)
Ref 548128Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022196)
Ref 548153Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022483)
Ref 548300Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024296)
Ref 548380Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025107)
Ref 548566Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026674)
Ref 548591Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026847)
Ref 548592Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026848)
Ref 548975Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031057)
Ref 549140Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032781)
Ref 550550Antidiabetic action of bezafibrate in a large observational database. Diabetes Care. 2009 Apr;32(4):547-51.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref
Ref 525897Pristanic acid and phytanic acid: naturally occurring ligands for the nuclear receptor peroxisome proliferator-activated receptor alpha. J Lipid Res. 2000 Nov;41(11):1801-7.
Ref 526054Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis. Bioorg Med Chem Lett. 2001 May 7;11(9):1225-7.
Ref 526192KRP-297, MCC-555. Nihon Rinsho. 2001 Nov;59(11):2200-6.
Ref 526404Cardiac function and metabolism in Type 2 diabetic mice after treatment with BM 17.0744, a novel PPAR-alpha activator. Am J Physiol Heart Circ Physiol. 2002 Sep;283(3):H949-57.
Ref 526582Bioorg Med Chem Lett. 2003 Apr 7;13(7):1277-80.Phenylacetic acid derivatives as hPPAR agonists.
Ref 526645MK-767. Kyorin/Banyu/Merck. Curr Opin Investig Drugs. 2003 Apr;4(4):444-8.
Ref 526707Bioorg Med Chem Lett. 2003 Oct 6;13(19):3185-90.O-arylmandelic acids as highly selective human PPAR alpha/gamma agonists.
Ref 526845Ragaglitazar: the pharmacokinetics, pharmacodynamics, and tolerability of a novel dual PPAR alpha and gamma agonist in healthy subjects and patients with type 2 diabetes. J Clin Pharmacol. 2003 Nov;43(11):1244-56.
Ref 526879J Med Chem. 2003 Nov 20;46(24):5121-4.Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.
Ref 526920A novel peroxisome proliferator-activated receptor alpha/gamma dual agonist demonstrates favorable effects on lipid homeostasis. Endocrinology. 2004 Apr;145(4):1640-8. Epub 2003 Dec 30.
Ref 527060Design and synthesis of alpha-aryloxy-alpha-methylhydrocinnamic acids: a novel class of dual peroxisome proliferator-activated receptor alpha/gamma agonists. J Med Chem. 2004 May 6;47(10):2422-5.
Ref 527076Antidiabetic and hypolipidemic potential of DRF 2519--a dual activator of PPAR-alpha and PPAR-gamma. Eur J Pharmacol. 2004 May 3;491(2-3):195-206.
Ref 527124A novel oxyiminoalkanoic acid derivative, TAK-559, activates human peroxisome proliferator-activated receptor subtypes. Eur J Pharmacol. 2004 Jul 8;495(1):17-26.
Ref 527135A new class of peroxisome proliferator-activated receptor agonists with a novel binding epitope shows antidiabetic effects. J Biol Chem. 2004 Sep 24;279(39):41124-30. Epub 2004 Jul 15.
Ref 527514A peroxisome proliferator-activated receptor alpha/gamma dual agonist with a unique in vitro profile and potent glucose and lipid effects in rodent models of type 2 diabetes and dyslipidemia. Mol Endocrinol. 2005 Jun;19(6):1593-605. Epub 2005 Apr 14.
Ref 527561Oleoylethanolamide, an endogenous PPAR-alpha agonist, lowers body weight and hyperlipidemia in obese rats. Neuropharmacology. 2005 Jun;48(8):1147-53. Epub 2005 Apr 21.
Ref 528458The disposition and metabolism of naveglitazar, a peroxisome proliferator-activated receptor alpha-gamma dual, gamma-dominant agonist in mice, rats, and monkeys. Drug Metab Dispos. 2007 Jan;35(1):51-61. Epub 2006 Sep 29.
Ref 529268A novel PPARalpha agonist ameliorates insulin resistance in dogs fed a high-fat diet. Am J Physiol Endocrinol Metab. 2008 May;294(5):E833-40.
Ref 529780Molecular characterization of novel and selective peroxisome proliferator-activated receptor alpha agonists with robust hypolipidemic activity in vivo. Mol Pharmacol. 2009 Feb;75(2):296-306.
Ref 529786Modulation of PPAR receptor subtype selectivity of the ligands: aliphatic chain vs aromatic ring as a spacer between pharmacophore and the lipophilic moiety. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6471-5.
Ref 529793Potent and selective PPAR-alpha agonist LY518674 upregulates both ApoA-I production and catabolism in human subjects with the metabolic syndrome. Arterioscler Thromb Vasc Biol. 2009 Jan;29(1):140-6.
Ref 529893Scaffold-based discovery of indeglitazar, a PPAR pan-active anti-diabetic agent. Proc Natl Acad Sci U S A. 2009 Jan 6;106(1):262-7.
Ref 530129Identification of a functional peroxisome proliferator-activated receptor (PPAR) response element (PPRE) in the human apolipoprotein A-IV gene. Biochem Pharmacol. 2009 Sep 1;78(5):523-30.
Ref 530192The peroxisome proliferator-activated receptor-alpha (PPAR-alpha) agonist, AVE8134, attenuates the progression of heart failure and increases survival in rats. Acta Pharmacol Sin. 2009 Jul;30(7):935-46.
Ref 530350J Med Chem. 2009 Aug 13;52(15):4631-9.Activation of peroxisome proliferator-activated receptor gamma (PPARgamma) by nitroalkene fatty acids: importance of nitration position and degree of unsaturation.
Ref 530777J Med Chem. 2010 Apr 8;53(7):2854-64.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).
Ref 531047Therapeutic potential of aleglitazar, a new dual PPAR-alpha/gamma agonist: implications for cardiovascular disease in patients with diabetes mellitus. Am J Cardiovasc Drugs. 2010;10(4):209-16.
Ref 531487Docking and molecular dynamics simulations of peroxisome proliferator activated receptors interacting with pan agonist sodelglitazar. Protein Pept Lett. 2011 Oct;18(10):1021-7.
Ref 531686Tolerability and pharmacokinetics of lobeglitazone (CKD-501), a peroxisome proliferator-activated receptor-gamma agonist: a single- and multiple-dose, double-blind, randomized control study in healthy male Korean subjects. Clin Ther. 2011 Nov;33(11):1819-30.
Ref 531722Discovery of cyclic amine-substituted benzoic acids as PPARalpha agonists. Bioorg Med Chem Lett. 2012 Jan 1;22(1):334-8.
Ref 531939Design novel dual agonists for treating type-2 diabetes by targeting peroxisome proliferator-activated receptors with core hopping approach. PLoS One. 2012;7(6):e38546.
Ref 532380Selective peroxisome proliferator-activated receptor alpha modulators (SPPARMalpha): the next generation of peroxisome proliferator-activated receptor alpha-agonists. Cardiovasc Diabetol. 2013 May 31;12:82.
Ref 532486Pharmacokinetics, safety, and tolerability of saroglitazar (ZYH1), a predominantly PPARalpha agonist with moderate PPARgamma agonist activity in healthy human subjects. Clin Drug Investig. 2013 Nov;33(11):809-16.
Ref 533647Differential activation of peroxisome proliferator-activated receptors by eicosanoids. J Biol Chem. 1995 Oct 13;270(41):23975-83.
Ref 534452PPAR alpha structure-function relationships derived from species-specific differences in responsiveness to hypolipidemic agents. Biol Chem. 1997 Jul;378(7):651-5.
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