Target Information
Target General Infomation | |||||
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Target ID |
T36557
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Former ID |
TTDC00069
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Target Name |
Peroxisomeproliferator activated receptor delta
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Gene Name |
PPARD
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Synonyms |
NUC1; NUCI; Nuclear hormone receptor 1; PPAR-beta; PPAR-delta; PPARdelta; Peroxisomeproliferator activated receptor beta/delta; Peroxisomeproliferator-activated receptor beta; PPARD
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Target Type |
Clinical Trial
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Disease | Atherosclerosis [ICD9: 414.0, 440; ICD10: I70] | ||||
Alzheimer disease [ICD9: 331; ICD10: G30] | |||||
Central nervous system disease [ICD10: G00-G99] | |||||
Dyslipidaemias [ICD9: 272; ICD10: E78] | |||||
Dyslipidaemias; Hyperlipidaemia; Obesity [ICD9:272, 272.0-272.4, 278; ICD10: E78, E66] | |||||
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 2 diabetes; Dyslipidemia [ICD9: 250, 250.00, 250.02, 272; ICD10: E08-E13, E11, E78] | |||||
Type 1 diabetes [ICD9: 250; ICD10: E10] | |||||
Type 2 diabetes [ICD9: 250; ICD10: E11] | |||||
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.
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BioChemical Class |
Zinc-finger
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Target Validation |
T36557
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UniProt ID | |||||
Sequence |
MEQPQEEAPEVREEEEKEEVAEAEGAPELNGGPQHALPSSSYTDLSRSSSPPSLLDQLQM
GCDGASCGSLNMECRVCGDKASGFHYGVHACEGCKGFFRRTIRMKLEYEKCERSCKIQKK NRNKCQYCRFQKCLALGMSHNAIRFGRMPEAEKRKLVAGLTANEGSQYNPQVADLKAFSK HIYNAYLKNFNMTKKKARSILTGKASHTAPFVIHDIETLWQAEKGLVWKQLVNGLPPYKE ISVHVFYRCQCTTVETVRELTEFAKSIPSFSSLFLNDQVTLLKYGVHEAIFAMLASIVNK DGLLVANGSGFVTREFLRSLRKPFSDIIEPKFEFAVKFNALELDDSDLALFIAAIILCGD RPGLMNVPRVEAIQDTILRALEFHLQANHPDAQYLFPKLLQKMADLRQLVTEHAQMMQRI KKTETETSLHPLLQEIYKDMY |
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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 522577 | ClinicalTrials.gov (NCT00841217) Regulation of Lipoprotein Transport in Metabolic Syndrome. U.S. National Institutes of Health. | ||||
Ref 525327 | ClinicalTrials.gov (NCT02560753) Feasibility Study in Subjects With Mild to Moderate Alzheimer's Disease. | ||||
Ref 536649 | Emerging 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 547644 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018093) | ||||
Ref 548153 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022483) | ||||
Ref 548328 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024671) | ||||
Ref 548380 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025107) | ||||
Ref 548591 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026847) | ||||
Ref 548750 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028321) | ||||
Ref 525344 | ClinicalTrials.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 525425 | Novel peroxisome proliferator-activated receptor (PPAR) gamma and PPARdelta ligands produce distinct biological effects. J Biol Chem. 1999 Mar 5;274(10):6718-25. | ||||
Ref 526582 | Bioorg Med Chem Lett. 2003 Apr 7;13(7):1277-80.Phenylacetic acid derivatives as hPPAR agonists. | ||||
Ref 526602 | Novel 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 529893 | Scaffold-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 530686 | J 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 531487 | Docking and molecular dynamics simulations of peroxisome proliferator activated receptors interacting with pan agonist sodelglitazar. Protein Pept Lett. 2011 Oct;18(10):1021-7. | ||||
Ref 534536 | Identification of peroxisome proliferator-activated receptor ligands from a biased chemical library. Chem Biol. 1997 Dec;4(12):909-18. | ||||
Ref 536649 | Emerging 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 544056 | Peroxisome Proliferators-Activated Receptor (PPAR) Modulators and Metabolic Disorders. PPAR Res. 2008; 2008: 679137. | ||||
Ref 544152 | Fibrates, glitazones, and peroxisome proliferator-activated receptors. Arterioscler Thromb Vasc Biol. 2010 May; 30(5): 894-899. | ||||
Ref 544477 | Addressing Unmet Medical Needs in Type 2 Diabetes: A Narrative Review of Drugs under Development. Curr Diabetes Rev. 2015 March; 11(1): 17-31. | ||||
Ref 550862 | CN patent application no. 102459215, 3-(4-aminophenyl)-2-furancarboxylic acid derivative and pharmaceutically acceptable salt thereof. | ||||
Ref 551391 | DrugBank 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 |
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