Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| 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 | |||||
|---|---|---|---|---|---|---|
| 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 | 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 | ||||
|---|---|---|---|---|---|
| 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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