Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T46456 | Target Info | |||
| Target Name | Retinoic acid receptor RXR-gamma (RXRG) | ||||
| Synonyms |
Retinoid X receptor gamma; Nuclear receptor subfamily 2 group B member 3; NR2B3
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| Target Type | Successful Target | ||||
| Gene Name | RXRG | ||||
| Biochemical Class | Nuclear hormone receptor | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Retinoic acid receptor RXR-alpha (RXRA) | Successful Target | ||||
| UniProt ID | RXRA_HUMAN | |||||
| Gene Name | RXRA | |||||
| Synonyms |
Retinoid X receptor alpha; RXRalpha; Nuclear receptor subfamily 2 group B member 1; NR2B1
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| Representative Drug(s) | IRX4204 | Drug Info | EC50 = 0.2 nM | Click to Show More | [1] | |
| 2 | Alitretinoin | Drug Info | EC50 = 1.5 nM | [1] | ||
| 3 | NRX-4204 | Drug Info | EC50 = 1.5 nM | [4] | ||
| 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 | [2] | |
| 2 | NRX-4204 | Drug Info | EC50 = 340 nM | [4] | ||
| 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) | IRX4204 | Drug Info | EC50 = 0.8 nM | Click to Show More | [1] | |
| 2 | NRX-4204 | Drug Info | EC50 = 2 nM | [4] | ||
| 3 | Alitretinoin | Drug Info | EC50 = 2.6 nM | [5] | ||
| 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 | [3] | |
| 2 | NRX-4204 | Drug Info | EC50 = 200 nM | [4] | ||
| 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) | IRX4204 | Drug Info | EC50 = 8.6 nM | [6] | ||
| 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) | Alitretinoin | Drug Info | IC50 = 7 nM | Click to Show More | [7] | |
| 2 | NRX-4204 | Drug Info | EC50 ~ 1000 nM | [4] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Enantioselective syntheses of potent retinoid X receptor ligands: differential biological activities of individual antipodes. J Med Chem. 2001 Jul 5;44(14):2298-303. | ||||
| REF 2 | Synthesis and receptor binding affinity of conformationally restricted retinoic acid analogues. Bioorg Med Chem Lett. 1997 Sep 9;7(17):2313-8. | ||||
| REF 3 | 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 4 | Synthesis of highly potent RXR-specific retinoids: The use of a cyclopropyl group as a double bond isostere. Bioorg Med Chem Lett. 1996 Jan 23;6(2):213-8. | ||||
| REF 5 | 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 6 | Design and synthesis of novel RXR-selective modulators with improved pharmacological profile. Bioorg Med Chem Lett. 2003 Nov 17;13(22):4071-5. | ||||
| REF 7 | 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. | ||||
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