Co-Target(s) Information
| Target General Information | Top | ||||
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| Target ID | T51426 | Target Info | |||
| Target Name | Farnesoid X-activated receptor (FXR) | ||||
| Synonyms |
Retinoid X receptor-interacting protein 14; RXR-interacting protein 14; RIP14; Nuclear receptor subfamily 1 group H member 4; HRR1; Farnesol receptor HRR-1; FXR; Bile acid receptor; BAR
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| Target Type | Successful Target | ||||
| Gene Name | NR1H4 | ||||
| Biochemical Class | Nuclear hormone receptor | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Mineralocorticoid receptor (MR) | Successful Target | ||||
| UniProt ID | MCR_HUMAN | |||||
| Gene Name | NR3C2 | |||||
| Synonyms |
Nuclear receptor subfamily 3 group C member 2; Mineralocorticoid receptor; MLR; MCR; Inner ear mineralocorticoid receptor; Delta
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| Representative Drug(s) | Guggulsterone | Drug Info | Ki = 37 nM | [1] | ||
| Co-Target Name | Progesterone receptor (PGR) | Successful Target | ||||
| UniProt ID | PRGR_HUMAN | |||||
| Gene Name | PGR | |||||
| Synonyms |
PR; Nuclear receptor subfamily 3 group C member 3; NR3C3
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| Representative Drug(s) | Guggulsterone | Drug Info | Ki = 224 nM | [1] | ||
| Co-Target Name | Glucocorticoid receptor (NR3C1) | Successful Target | ||||
| UniProt ID | GCR_HUMAN | |||||
| Gene Name | NR3C1 | |||||
| Synonyms |
Nuclear receptor subfamily 3 group C member 1; GRL; GR
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| Representative Drug(s) | Guggulsterone | Drug Info | Ki = 252 nM | [1] | ||
| Co-Target Name | Androgen receptor (AR) | Successful Target | ||||
| UniProt ID | ANDR_HUMAN | |||||
| Gene Name | AR | |||||
| Synonyms |
Testosterone receptor; Nuclear receptor subfamily 3 group C member 4; NR3C4; Dihydrotestosterone receptor; DHTR
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| Representative Drug(s) | Guggulsterone | Drug Info | Ki = 315 nM | [1] | ||
| Co-Target Name | G-protein coupled bile acid receptor 1 (GPBAR1) | Clinical trial Target | ||||
| UniProt ID | GPBAR_HUMAN | |||||
| Gene Name | GPBAR1 | |||||
| Synonyms |
hGPCR19; hBG37; TGR5; Membrane-type receptor for bile acids; M-BAR; G-protein coupled receptor GPCR19; BG37
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| Representative Drug(s) | obeticholic acid | Drug Info | EC50 = 100 nM | Click to Show More | [2] | |
| 2 | Bevacizumab + Trastuzumab | Drug Info | EC50 = 580 nM | [3] | ||
| Co-Target Name | Pregnane X receptor (NR1I2) | Literature-reported Target | ||||
| UniProt ID | NR1I2_HUMAN | |||||
| Gene Name | NR1I2 | |||||
| Synonyms |
Steroid and xenobiotic receptor; SXR; PXR; Orphan nuclear receptor PXR; Orphan nuclear receptor PAR1; Nuclear receptor subfamily 1 group I member 2
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| Representative Drug(s) | Guggulsterone | Drug Info | IC50 = 2.4 nM | [1] | ||
| References | Top | ||||
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| REF 1 | Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. J Med Chem. 2005 Nov 3;48(22):6948-55. | ||||
| REF 2 | Probing the Binding Site of Bile Acids in TGR5. ACS Med Chem Lett. 2013 Oct 15;4(12):1158-62. | ||||
| REF 3 | Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies. J Med Chem. 2008 Mar 27;51(6):1831-41. | ||||
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