Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T13726 | Target Info | |||
| Target Name | Retinoic acid receptor RXR-alpha (RXRA) | ||||
| Synonyms |
Retinoid X receptor alpha; RXRalpha; Nuclear receptor subfamily 2 group B member 1; NR2B1
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| Target Type | Successful Target | ||||
| Gene Name | RXRA | ||||
| Biochemical Class | Nuclear hormone receptor | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Retinoic acid receptor beta (RARB) | Successful Target | ||||
| UniProt ID | RARB_HUMAN | |||||
| Gene Name | RARB | |||||
| Synonyms |
RAR-epsilon; RAR-beta; Nuclear receptor subfamily 1 group B member 2; NR1B2; HBV-activated protein; HAP
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| Representative Drug(s) | Alitretinoin | Drug Info | Ki = 0.5 nM | Click to Show More | [1] | |
| 2 | Bexarotene | Drug Info | Ki = 50 nM | [2] | ||
| Co-Target Name | Retinoic acid receptor gamma (RARG) | Successful Target | ||||
| UniProt ID | RARG_HUMAN | |||||
| Gene Name | RARG | |||||
| Synonyms |
RAR-gamma; Nuclear receptor subfamily 1 group B member 3; NR1B3
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| Representative Drug(s) | Alitretinoin | Drug Info | Ki = 1 nM | Click to Show More | [2] | |
| 2 | Bexarotene | Drug Info | Ki = 130 nM | [2] | ||
| Co-Target Name | Retinoic acid receptor RXR-beta (RXRB) | Successful Target | ||||
| UniProt ID | RXRB_HUMAN | |||||
| Gene Name | RXRB | |||||
| Synonyms |
Retinoid X receptor beta; Nuclear receptor subfamily 2 group B member 2; NR2B2
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| Representative Drug(s) | Alitretinoin | Drug Info | EC50 = 2.6 nM | Click to Show More | [3] | |
| 2 | Bexarotene | Drug Info | Ki = 5.9 nM | [2] | ||
| Co-Target Name | Retinoic acid receptor RXR-gamma (RXRG) | Successful Target | ||||
| UniProt ID | RXRG_HUMAN | |||||
| Gene Name | RXRG | |||||
| Synonyms |
Retinoid X receptor gamma; Nuclear receptor subfamily 2 group B member 3; NR2B3
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| Representative Drug(s) | Alitretinoin | Drug Info | IC50 = 4 nM | Click to Show More | [4] | |
| 2 | Bexarotene | Drug Info | Ki = 8.3 nM | [2] | ||
| Co-Target Name | Retinoic acid receptor alpha (RARA) | Clinical trial Target | ||||
| UniProt ID | RARA_HUMAN | |||||
| Gene Name | RARA | |||||
| Synonyms |
RAR-alpha; RAR alpha; Nuclear receptor subfamily 1 group B member 1; NR1B1
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| Representative Drug(s) | Bexarotene | Drug Info | EC50 = 6 nM | Click to Show More | [5] | |
| 2 | Alitretinoin | Drug Info | IC50 = 7 nM | [4] | ||
| Co-Target Name | Oxysterols receptor LXR-beta (NR1H2) | Clinical trial Target | ||||
| UniProt ID | NR1H2_HUMAN | |||||
| Gene Name | NR1H2 | |||||
| Synonyms |
Ubiquitously-expressed nuclear receptor; Nuclear receptor subfamily 1 group H member 2; Nuclear receptor NER; Nuclear orphan receptor LXR-beta; NER; Liver X receptor beta; LXRbeta; LXRB
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| Representative Drug(s) | Bexarotene | Drug Info | EC50 = 434 nM | [6] | ||
| Co-Target Name | Oxysterols receptor LXR-alpha (NR1H3) | Patented-recorded Target | ||||
| UniProt ID | NR1H3_HUMAN | |||||
| Gene Name | NR1H3 | |||||
| Synonyms |
Nuclear receptor subfamily 1 group H member 3; Nuclear receptor LXRalpha; Nuclear orphan receptor LXR-alpha; Liver X receptor alpha; LXRalpha; LXRA
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| Representative Drug(s) | Bexarotene | Drug Info | EC50 = 196 nM | [6] | ||
| Co-Target Name | Nuclear receptor 4A2-Retinoic acid receptor RXR alpha complex (NR4A2-RXRA) | Co-Target | ||||
| UniProt ID | NR4A2_HUMAN-RXRA_HUMAN | |||||
| Gene Name | NR4A2-RXRA | |||||
| Representative Drug(s) | Bexarotene | Drug Info | EC50 = 10 nM | [7] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Synthesis and receptor binding affinity of conformationally restricted retinoic acid analogues. Bioorg Med Chem Lett. 1997 Sep 9;7(17):2313-8. | ||||
| REF 2 | Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers. J Med Chem. 1997 Dec 19;40(26):4222-34. | ||||
| REF 3 | Conformational effects on retinoid receptor selectivity. 2. Effects of retinoid bridging group on retinoid X receptor activity and selectivity. J Med Chem. 1995 Aug 18;38(17):3368-83. | ||||
| REF 4 | Synthesis of high specific activity [3H]-9-cis-retinoic acid and its application for identifying retinoids with unusual binding properties. J Med Chem. 1994 Feb 4;37(3):408-14. | ||||
| REF 5 | Synthesis of retinoid X receptor-specific ligands that are potent inducers of adipogenesis in 3T3-L1 cells. J Med Chem. 1999 Feb 25;42(4):742-50. | ||||
| REF 6 | DrugBank screening revealed alitretinoin and bexarotene as liver X receptor modulators. Bioorg Med Chem Lett. 2017 Mar 1;27(5):1193-8. | ||||
| REF 7 | Chiral Dihydrobenzofuran Acids Show Potent Retinoid X Receptor-Nuclear Receptor Related 1 Protein Dimer Activation. J Med Chem. 2016 Feb 11;59(3):1232-8. | ||||
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