Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T86591 | Target Info | |||
Target Name | Peroxisome proliferator-activated receptor alpha (PPARA) | ||||
Synonyms |
Peroxisome proliferater-activated receptor alpha; PPARalpha; PPAR-alpha; PPAR; Nuclear receptor subfamily 1 group C member 1; NR1C1
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Target Type | Successful Target | ||||
Gene Name | PPARA | ||||
Biochemical Class | Nuclear hormone receptor | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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Co-Target Name | Peroxisome proliferator-activated receptor gamma (PPAR-gamma) | Successful Target | ||||
UniProt ID | PPARG_HUMAN | |||||
Gene Name | PPARG | |||||
Synonyms |
PPAR-gamma; Nuclear receptor subfamily 1 group C member 3; NR1C3
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Representative Drug(s) | GW-409544 | Drug Info | EC50 = 0.2 nM | Click to Show More | [1] | |
2 | MURAGLITAZAR | Drug Info | EC50 = 3 nM | [2] | ||
3 | Imiglitazar | Drug Info | EC50 = 4 nM | [3] | ||
4 | TESAGLITAZAR | Drug Info | EC50 = 13 nM | [4] | ||
5 | Naveglitazar | Drug Info | IC50 = 33.96 nM | [5] | ||
6 | Ragaglitazar | Drug Info | Ki = 90 nM | [1] | ||
7 | Fenofibrate | Drug Info | EC50 = 570 nM | [6] | ||
Co-Target Name | Peroxisome proliferator-activated receptor delta (PPARD) | Clinical trial Target | ||||
UniProt ID | PPARD_HUMAN | |||||
Gene Name | PPARD | |||||
Synonyms |
Peroxisomeproliferator-activated receptor beta; Peroxisomeproliferator activated receptor beta/delta; Peroxisome proliferator-activated receptor beta; PPARdelta; PPARB; PPAR-delta; PPAR-beta; Nuclear receptor subfamily 1 group C member 2; Nuclear hormone receptor 1; NUCI; NUC1; NR1C2
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Representative Drug(s) | GFT-505 | Drug Info | EC50 = 10 nM | [7] |
References | Top | ||||
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REF 1 | Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes. J Med Chem. 2004 Aug 12;47(17):4118-27. | ||||
REF 2 | Anti-diabetic activity of fused PPARgamma-SIRT1 ligands with limited body-weight gain by mimicking calorie restriction and decreasing SGK1 expression. Eur J Med Chem. 2017 Sep 8;137:310-26. | ||||
REF 3 | Modulation 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 4 | Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5586-90. | ||||
REF 5 | Activity landscape modeling of PPAR ligands with dual-activity difference maps. Bioorg Med Chem. 2012 Jun 1;20(11):3523-32. | ||||
REF 6 | Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template. Bioorg Med Chem Lett. 2003 Jan 20;13(2):257-60. | ||||
REF 7 | The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease. J Med Chem. 2020 May 28;63(10):5031-5073. |
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