Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| 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; 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 disease; Obesity [ICD9: 270-279, 278; ICD10: E66, E70-E89] | |||||
| Metabolic disorders [ICD9: 270-279; ICD10: 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 | [1] |
| GFT-505 | Drug Info | Phase 2 | Type 2 diabetes | [2] | |
| T3D-959 | Drug Info | Phase 1/2 | Alzheimer disease | [3] | |
| CER-002 | Drug Info | Phase 1 | Dyslipidaemias | [4] | |
| KD3010 | Drug Info | Phase 1 | Metabolic disease; Obesity | [5] | |
| SAR351034 | Drug Info | Phase 1 | Type 2 diabetes; Dyslipidemia | [6] | |
| KD-3020 | Drug Info | Preclinical | Non-alcoholic fatty liver disease | [7] | |
| GW-501516 | Drug Info | Discontinued in Phase 4 | Type 1 diabetes | [8], [9] | |
| GSK-677954 | Drug Info | Discontinued in Phase 2 | Non-alcoholic fatty liver disease | [7] | |
| Indeglitazar | Drug Info | Discontinued in Phase 2 | Type 2 diabetes | [10] | |
| Sodelglitazar | Drug Info | Discontinued in Phase 2 | Hyperlipidaemia | [11] | |
| CS-204 | Drug Info | Terminated | Metabolic disorders | [12] | |
| Inhibitor | (11E)-OCTADEC-11-ENOIC ACID | Drug Info | [13] | ||
| GSK-0660 | Drug Info | [14] | |||
| GSK-3787 | Drug Info | [14] | |||
| Heptyl-Beta-D-Glucopyranoside | Drug Info | [13] | |||
| L-165461 | Drug Info | [15] | |||
| L-796449 | Drug Info | [15] | |||
| Agonist | CER-002 | Drug Info | [16] | ||
| CS-204 | Drug Info | [17] | |||
| DB-900 | Drug Info | [18] | |||
| GSK-677954 | Drug Info | [7] | |||
| GW0742X | Drug Info | [19] | |||
| GW2433 | Drug Info | [20] | |||
| Indeglitazar | Drug Info | [21] | |||
| KD-3020 | Drug Info | [7] | |||
| KD3010 | Drug Info | [5] | |||
| L-165041 | Drug Info | [22] | |||
| L-783483 | Drug Info | [22] | |||
| MBX-8025 | Drug Info | [23] | |||
| PPAR delta agonists | Drug Info | [24] | |||
| Sodelglitazar | Drug Info | [25] | |||
| Modulator | GFT-505 | Drug Info | |||
| GW-501516 | Drug Info | ||||
| SAR351034 | Drug Info | [26] | |||
| SAVX-1 | Drug Info | [24] | |||
| 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 1 | 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 2 | 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 3 | ClinicalTrials.gov (NCT02560753) Feasibility Study in Subjects With Mild to Moderate Alzheimer's Disease. | ||||
| REF 4 | 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 5 | Kalypsys nearing completion of phase Ia study of KD3010 for metabolic disorders. Kalypsys. 2007. | ||||
| REF 6 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029833) | ||||
| REF 7 | Emerging drugs for non-alcoholic fatty liver disease. Expert Opin Emerg Drugs. 2008 Mar;13(1):145-58. | ||||
| REF 8 | ClinicalTrials.gov (NCT00841217) Regulation of Lipoprotein Transport in Metabolic Syndrome. U.S. National Institutes of Health. | ||||
| REF 9 | (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 10 | 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 11 | 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 12 | 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 13 | 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 | ||||
| REF 14 | 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 15 | Bioorg Med Chem Lett. 2003 Apr 7;13(7):1277-80.Phenylacetic acid derivatives as hPPAR agonists. | ||||
| REF 16 | Fibrates, glitazones, and peroxisome proliferator-activated receptors. Arterioscler Thromb Vasc Biol. 2010 May; 30(5): 894-899. | ||||
| REF 17 | Peroxisome Proliferators-Activated Receptor (PPAR) Modulators and Metabolic Disorders. PPAR Res. 2008; 2008: 679137. | ||||
| REF 18 | CN patent application no. 102459215, 3-(4-aminophenyl)-2-furancarboxylic acid derivative and pharmaceutically acceptable salt thereof. | ||||
| REF 19 | 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 20 | Identification of peroxisome proliferator-activated receptor ligands from a biased chemical library. Chem Biol. 1997 Dec;4(12):909-18. | ||||
| REF 21 | 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 22 | 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 23 | 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 24 | (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 25 | 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 26 | Addressing Unmet Medical Needs in Type 2 Diabetes: A Narrative Review of Drugs under Development. Curr Diabetes Rev. 2015 March; 11(1): 17-31. | ||||
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