Target Information
Target General Information | Top | |||||
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Target ID |
T46456
(Former ID: TTDR01075)
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Target Name |
Retinoic acid receptor RXR-gamma (RXRG)
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Synonyms |
Retinoid X receptor gamma; Nuclear receptor subfamily 2 group B member 3; NR2B3
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Gene Name |
RXRG
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 2 Target-related Diseases | + | ||||
1 | Kaposi sarcoma [ICD-11: 2B57] | |||||
2 | Light sensitivity impairment [ICD-11: 9D45] | |||||
Function |
Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RAR/RXR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. The high affinity ligand for RXRs is 9-cis retinoic acid. Receptor for retinoic acid.
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BioChemical Class |
Nuclear hormone receptor
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UniProt ID | ||||||
Sequence |
MYGNYSHFMKFPAGYGGSPGHTGSTSMSPSAALSTGKPMDSHPSYTDTPVSAPRTLSAVG
TPLNALGSPYRVITSAMGPPSGALAAPPGINLVAPPSSQLNVVNSVSSSEDIKPLPGLPG IGNMNYPSTSPGSLVKHICAICGDRSSGKHYGVYSCEGCKGFFKRTIRKDLIYTCRDNKD CLIDKRQRNRCQYCRYQKCLVMGMKREAVQEERQRSRERAESEAECATSGHEDMPVERIL EAELAVEPKTESYGDMNMENSTNDPVTNICHAADKQLFTLVEWAKRIPHFSDLTLEDQVI LLRAGWNELLIASFSHRSVSVQDGILLATGLHVHRSSAHSAGVGSIFDRVLTELVSKMKD MQMDKSELGCLRAIVLFNPDAKGLSNPSEVETLREKVYATLEAYTKQKYPEQPGRFAKLL LRLPALRSIGLKCLEHLFFFKLIGDTPIDTFLMEMLETPLQIT Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 2 Approved Drugs | + | ||||
1 | Alitretinoin | Drug Info | Approved | Kaposi sarcoma | [2], [3] | |
2 | Vitamin A | Drug Info | Approved | Night blindness | [1], [4] | |
Clinical Trial Drug(s) | [+] 3 Clinical Trial Drugs | + | ||||
1 | NRX-4204 | Drug Info | Phase 2 | Diabetic complication | [5], [6] | |
2 | 9cUAB-30 | Drug Info | Phase 1 | Solid tumour/cancer | [7] | |
3 | IRX4204 | Drug Info | Phase 1 | Prostate cancer | [8] | |
Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
1 | SR-11237 | Drug Info | Terminated | Solid tumour/cancer | [9], [10] | |
Mode of Action | [+] 5 Modes of Action | + | ||||
Agonist | [+] 1 Agonist drugs | + | ||||
1 | Alitretinoin | Drug Info | [11] | |||
Binder | [+] 1 Binder drugs | + | ||||
1 | Vitamin A | Drug Info | [1] | |||
Modulator | [+] 4 Modulator drugs | + | ||||
1 | NRX-4204 | Drug Info | [12] | |||
2 | 9cUAB-30 | Drug Info | [7] | |||
3 | IRX4204 | Drug Info | [13] | |||
4 | SR-11237 | Drug Info | [14] | |||
Inhibitor | [+] 1 Inhibitor drugs | + | ||||
1 | AGN-34 | Drug Info | [15] | |||
Antagonist | [+] 1 Antagonist drugs | + | ||||
1 | LG100754 | Drug Info | [16] |
Chemical Structure based Activity Landscape of Target | Top |
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Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Co-Targets | Top | |||||
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Co-Targets |
Target Poor or Non Binders | Top | |||||
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Target Poor or Non Binders |
Target Regulators | Top | |||||
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Target-regulating Transcription Factors | ||||||
Target-interacting Proteins |
Target Profiles in Patients | Top | |||||
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Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
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KEGG Pathway | [+] 8 KEGG Pathways | + | ||||
1 | PPAR signaling pathway | |||||
2 | Thyroid hormone signaling pathway | |||||
3 | Adipocytokine signaling pathway | |||||
4 | Pathways in cancer | |||||
5 | Transcriptional misregulation in cancer | |||||
6 | Thyroid cancer | |||||
7 | Small cell lung cancer | |||||
8 | Non-small cell lung cancer | |||||
PID Pathway | [+] 4 PID Pathways | + | ||||
1 | Regulation of Androgen receptor activity | |||||
2 | RXR and RAR heterodimerization with other nuclear receptor | |||||
3 | Retinoic acid receptors-mediated signaling | |||||
4 | a6b1 and a6b4 Integrin signaling | |||||
Reactome | [+] 1 Reactome Pathways | + | ||||
1 | Nuclear Receptor transcription pathway | |||||
WikiPathways | [+] 3 WikiPathways | + | ||||
1 | Vitamin A and Carotenoid Metabolism | |||||
2 | Adipogenesis | |||||
3 | Nuclear Receptors |
Target-Related Models and Studies | Top | |||||
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Target Validation |
References | Top | |||||
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REF 1 | Vitamins and cofactors: highlights of ESBOC 2009. Nat Chem Biol. 2009 Aug;5(8):530-3. | |||||
REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2645). | |||||
REF 3 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
REF 4 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4053). | |||||
REF 5 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2811). | |||||
REF 6 | ClinicalTrials.gov (NCT01540071) Trial of NRX 194204 in Castration- and Taxane-Resistant Prostate Cancer. U.S. National Institutes of Health. | |||||
REF 7 | In vitro metabolic characterization, phenotyping, and kinetic studies of 9cUAB30, a retinoid X receptor-specific retinoid. Drug Metab Dispos. 2007 Jul;35(7):1157-64. | |||||
REF 8 | ClinicalTrials.gov (NCT02438215) Study of IRX4204 for Treatment of Early Parkinson's Disease. U.S. National Institutes of Health. | |||||
REF 9 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2809). | |||||
REF 10 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005745) | |||||
REF 11 | Retinoic acid receptors and retinoid X receptors: interactions with endogenous retinoic acids. Proc Natl Acad Sci U S A. 1993 Jan 1;90(1):30-4. | |||||
REF 12 | DOI: 10.1038/scibx.2010.766 | |||||
REF 13 | Selective brain penetrable Nurr1 transactivator for treating Parkinson's disease.Oncotarget.2016 Feb 16;7(7):7469-79. | |||||
REF 14 | Silicon analogues of the RXR-selective retinoid agonist SR11237 (BMS649): chemistry and biology. ChemMedChem. 2009 Jul;4(7):1143-52. | |||||
REF 15 | Farnesoid X receptor: from structure to potential clinical applications. J Med Chem. 2005 Aug 25;48(17):5383-403. | |||||
REF 16 | Activation of specific RXR heterodimers by an antagonist of RXR homodimers. Nature. 1996 Oct 3;383(6599):450-3. |
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