Target Information

Target General Infomation
Target ID
T36557
Former ID
TTDC00069
Target Name
Peroxisomeproliferator activated receptor delta
Gene Name
PPARD
Synonyms
NUC1; NUCI; Nuclear hormone receptor 1; PPAR-beta; PPAR-delta; PPARdelta; Peroxisomeproliferator activated receptor beta/delta; Peroxisomeproliferator-activated receptor beta; PPARD
Target Type
Clinical Trial
Disease Alzheimer disease [ICD9: 331; ICD10: G30]
Atherosclerosis [ICD9: 414.0, 440; ICD10: I70]
Central nervous system disease [ICD10: G00-G99]
Dyslipidaemias; Hyperlipidaemia; Obesity [ICD9:272, 272.0-272.4, 278; ICD10: E78, E66]
Dyslipidaemias [ICD9: 272; ICD10: E78]
Hyperlipidaemia [ICD9: 272.0-272.4; ICD10: E78]
Metabolic disorders [ICD9: 270-279; ICD10: E70-E89]
Metabolic disease; Obesity [ICD9: 270-279, 278; ICD10: E66, E70-E89]
Non-alcoholic fatty liver disease [ICD9: 571.8; ICD10: K76.0]
Type 1 diabetes [ICD9: 250; ICD10: E10]
Type 2 diabetes [ICD9: 250; ICD10: E11]
Type 2 diabetes; Dyslipidemia [ICD9: 250, 250.00, 250.02, 272; ICD10: E08-E13, E11, E78]
Function
Receptor that bind peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the receptor binds to a promoter element in the gene for acyl-coa oxidase and activates its transcription.
BioChemical Class
Zinc-finger
Target Validation
T36557
UniProt ID
Q03181
Sequence
MEQPQEEAPEVREEEEKEEVAEAEGAPELNGGPQHALPSSSYTDLSRSSSPPSLLDQLQM
GCDGASCGSLNMECRVCGDKASGFHYGVHACEGCKGFFRRTIRMKLEYEKCERSCKIQKK
NRNKCQYCRFQKCLALGMSHNAIRFGRMPEAEKRKLVAGLTANEGSQYNPQVADLKAFSK
HIYNAYLKNFNMTKKKARSILTGKASHTAPFVIHDIETLWQAEKGLVWKQLVNGLPPYKE
ISVHVFYRCQCTTVETVRELTEFAKSIPSFSSLFLNDQVTLLKYGVHEAIFAMLASIVNK
DGLLVANGSGFVTREFLRSLRKPFSDIIEPKFEFAVKFNALELDDSDLALFIAAIILCGD
RPGLMNVPRVEAIQDTILRALEFHLQANHPDAQYLFPKLLQKMADLRQLVTEHAQMMQRI
KKTETETSLHPLLQEIYKDMY
Drugs and Mode of Action
Drug(s) MBX-8025 Drug Info Phase 2/3 Dyslipidaemias; Hyperlipidaemia; Obesity [548328]
GFT-505 Drug Info Phase 2 Type 2 diabetes [548380]
T3D-959 Drug Info Phase 1/2 Alzheimer disease [525327]
CER-002 Drug Info Phase 1 Dyslipidaemias [548750]
KD3010 Drug Info Phase 1 Metabolic disease; Obesity [551433]
SAR351034 Drug Info Phase 1 Type 2 diabetes; Dyslipidemia [548882]
KD-3020 Drug Info Preclinical Non-alcoholic fatty liver disease [536649]
GW-501516 Drug Info Discontinued in Phase 4 Type 1 diabetes [522577], [539749]
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]
Sodelglitazar Drug Info Discontinued in Phase 2 Hyperlipidaemia [547644]
CS-204 Drug Info Terminated Metabolic disorders [548591]
Inhibitor (11E)-OCTADEC-11-ENOIC ACID Drug Info [551391]
GSK-0660 Drug Info [530686]
GSK-3787 Drug Info [530686]
Heptyl-Beta-D-Glucopyranoside Drug Info [551391]
L-165461 Drug Info [526582]
L-796449 Drug Info [526582]
Agonist CER-002 Drug Info [544152]
CS-204 Drug Info [544056]
DB-900 Drug Info [550862]
GSK-677954 Drug Info [536649]
GW0742X Drug Info [526602]
GW2433 Drug Info [534536]
Indeglitazar Drug Info [529893]
KD-3020 Drug Info [536649]
KD3010 Drug Info [551433]
L-165041 Drug Info [525425]
L-783483 Drug Info [525425]
MBX-8025 Drug Info [525344]
PPAR delta agonists Drug Info [543890]
Sodelglitazar Drug Info [531487]
Modulator GFT-505 Drug Info
GW-501516 Drug Info
SAR351034 Drug Info [544477]
SAVX-1 Drug Info [543890]
T3D-959 Drug Info
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway PPAR signaling pathway
Wnt signaling pathway
Pathways in cancer
Acute myeloid leukemia
NetPath Pathway IL2 Signaling Pathway
PANTHER Pathway Wnt signaling pathway
Pathway Interaction Database Presenilin action in Notch and Wnt signaling
RXR and RAR heterodimerization with other nuclear receptor
Reactome Import of palmitoyl-CoA into the mitochondrial matrix
Regulation of pyruvate dehydrogenase (PDH) complex
Nuclear Receptor transcription pathway
WikiPathways Wnt Signaling Pathway and Pluripotency
Nuclear Receptors in Lipid Metabolism and Toxicity
NRF2 pathway
Nuclear Receptors Meta-Pathway
Vitamin D Receptor Pathway
Ectoderm Differentiation
Adipogenesis
Nuclear Receptors
References
Ref 522577ClinicalTrials.gov (NCT00841217) Regulation of Lipoprotein Transport in Metabolic Syndrome. U.S. National Institutes of Health.
Ref 525327ClinicalTrials.gov (NCT02560753) Feasibility Study in Subjects With Mild to Moderate Alzheimer's Disease.
Ref 536649Emerging drugs for non-alcoholic fatty liver disease. Expert Opin Emerg Drugs. 2008 Mar;13(1):145-58.
Ref 539749(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: 2687).
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 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 548328Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024671)
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 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 548750Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028321)
Ref 548882Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029833)
Ref 551433Kalypsys nearing completion of phase Ia study of KD3010 for metabolic disorders. Kalypsys. 2007.
Ref 525344ClinicalTrials.gov (NCT00701883) Safety and Benefit of MBX-8025 With and Without Commonly Used Statins in Moderately Overweight Patients With High Cholesterol. U. S. National Institute of Health. 2008.
Ref 525425Novel peroxisome proliferator-activated receptor (PPAR) gamma and PPARdelta ligands produce distinct biological effects. J Biol Chem. 1999 Mar 5;274(10):6718-25.
Ref 526582Bioorg Med Chem Lett. 2003 Apr 7;13(7):1277-80.Phenylacetic acid derivatives as hPPAR agonists.
Ref 526602Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity. Bioorg Med Chem Lett. 2003 May 5;13(9):1517-21.
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 530686J Med Chem. 2010 Feb 25;53(4):1857-61.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.
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 534536Identification of peroxisome proliferator-activated receptor ligands from a biased chemical library. Chem Biol. 1997 Dec;4(12):909-18.
Ref 536649Emerging drugs for non-alcoholic fatty liver disease. Expert Opin Emerg Drugs. 2008 Mar;13(1):145-58.
Ref 543890(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. (Target id: 594).
Ref 544056Peroxisome Proliferators-Activated Receptor (PPAR) Modulators and Metabolic Disorders. PPAR Res. 2008; 2008: 679137.
Ref 544152Fibrates, glitazones, and peroxisome proliferator-activated receptors. Arterioscler Thromb Vasc Biol. 2010 May; 30(5): 894-899.
Ref 544477Addressing Unmet Medical Needs in Type 2 Diabetes: A Narrative Review of Drugs under Development. Curr Diabetes Rev. 2015 March; 11(1): 17-31.
Ref 550862CN patent application no. 102459215, 3-(4-aminophenyl)-2-furancarboxylic acid derivative and pharmaceutically acceptable salt thereof.
Ref 551391DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-4. Nucleic Acids Res. 2011 January
Ref 551433Kalypsys nearing completion of phase Ia study of KD3010 for metabolic disorders. Kalypsys. 2007.
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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