Target Information
Target General Infomation | |||||
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Target ID |
T13726
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Former ID |
TTDR01073
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Target Name |
Retinoic acid receptor RXR-alpha
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Gene Name |
RXRA
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Synonyms |
RXRalpha; RXRA
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Target Type |
Successful
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Disease | Cutaneous T-cell lymphoma [ICD9: 202.1, 202.2; ICD10: C84.0, C84.1] | ||||
Function |
Receptor for retinoic acid. 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. RXRA serves as a common heterodimeric partner for a number of nuclear receptors. The RXR/RAR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3'sites known as DR1-DR5. In the absence of ligand, the RXR-RAR heterodimers associate with a multiprotein complex containing transcription corepressors that induce histone acetylation, chromatin condensation and transcriptional suppression. On ligand binding, the corepressors dissociate from the receptors and associate with the coactivators leading to transcriptional activation. The RXRA/PPARA heterodimer is required for PPARA transcriptional activity on fatty acid oxidation genes such as ACOX1 and the P450 system genes.
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BioChemical Class |
Zinc-finger
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Target Validation |
T13726
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UniProt ID | |||||
Sequence |
MDTKHFLPLDFSTQVNSSLTSPTGRGSMAAPSLHPSLGPGIGSPGQLHSPISTLSSPING
MGPPFSVISSPMGPHSMSVPTTPTLGFSTGSPQLSSPMNPVSSSEDIKPPLGLNGVLKVP AHPSGNMASFTKHICAICGDRSSGKHYGVYSCEGCKGFFKRTVRKDLTYTCRDNKDCLID KRQRNRCQYCRYQKCLAMGMKREAVQEERQRGKDRNENEVESTSSANEDMPVERILEAEL AVEPKTETYVEANMGLNPSSPNDPVTNICQAADKQLFTLVEWAKRIPHFSELPLDDQVIL LRAGWNELLIASFSHRSIAVKDGILLATGLHVHRNSAHSAGVGAIFDRVLTELVSKMRDM QMDKTELGCLRAIVLFNPDSKGLSNPAEVEALREKVYASLEAYCKHKYPEQPGRFAKLLL RLPALRSIGLKCLEHLFFFKLIGDTPIDTFLMEMLEAPHQMT |
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Drugs and Mode of Action | |||||
Inhibitor | (5BETA)-PREGNANE-3,20-DIONE | Drug Info | [551374] | ||
2-chloro-5-nitro-N-phenylbenzamide | Drug Info | [551374] | |||
AGN-34 | Drug Info | [527690] | |||
Tributylstannanyl | Drug Info | [551374] | |||
Modulator | Bexarotene | Drug Info | [556264] | ||
Agonist | CD3254 | Drug Info | [526251] | ||
methoprene acid | Drug Info | [533651] | |||
phytanic acid | Drug Info | [534113] | |||
[3H]9-cis-retinoic acid | Drug Info | [534000] | |||
Antagonist | LG100754 | Drug Info | [526108] | ||
PA451 | Drug Info | [526387] | |||
UVI3003 | Drug Info | [527278] | |||
Pathways | |||||
KEGG Pathway | PPAR signaling pathway | ||||
PI3K-Akt signaling pathway | |||||
Thyroid hormone signaling pathway | |||||
Adipocytokine signaling pathway | |||||
Non-alcoholic fatty liver disease (NAFLD) | |||||
Bile secretion | |||||
Hepatitis C | |||||
Pathways in cancer | |||||
Transcriptional misregulation in cancer | |||||
Thyroid cancer | |||||
Small cell lung cancer | |||||
Non-small cell lung cancer | |||||
PANTHER Pathway | Vitamin D metabolism and pathway | ||||
Pathway Interaction Database | Regulation of Androgen receptor activity | ||||
RXR and RAR heterodimerization with other nuclear receptor | |||||
Retinoic acid receptors-mediated signaling | |||||
a6b1 and a6b4 Integrin signaling | |||||
Reactome | RORA activates gene expression | ||||
CLOCK,NPAS2 activates circadian gene expression | |||||
Recycling of bile acids and salts | |||||
PPARA activates gene expression | |||||
Import of palmitoyl-CoA into the mitochondrial matrix | |||||
YAP1- and WWTR1 (TAZ)-stimulated gene expression | |||||
Regulation of pyruvate dehydrogenase (PDH) complex | |||||
Endogenous sterols | |||||
Transcriptional activation of mitochondrial biogenesis | |||||
Activation of gene expression by SREBF (SREBP) | |||||
Transcriptional regulation of white adipocyte differentiation | |||||
Nuclear Receptor transcription pathway | |||||
Regulation of lipid metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha) | |||||
Circadian Clock | |||||
WikiPathways | Vitamin A and Carotenoid Metabolism | ||||
NRF2 pathway | |||||
Nuclear Receptors Meta-Pathway | |||||
Farnesoid X Receptor Pathway | |||||
PPAR Alpha Pathway | |||||
Vitamin D Receptor Pathway | |||||
Pregnane X Receptor pathway | |||||
Constitutive Androstane Receptor Pathway | |||||
Liver X Receptor Pathway | |||||
Regulation of Lipid Metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha) | |||||
Transcriptional Regulation of White Adipocyte Differentiation | |||||
YAP1- and WWTR1 (TAZ)-stimulated gene expression | |||||
Activation of Gene Expression by SREBP (SREBF) | |||||
Integrated Pancreatic Cancer Pathway | |||||
Adipogenesis | |||||
Circadian Clock | |||||
Nuclear Receptors | |||||
Vitamin D Metabolism | |||||
References | |||||
Ref 526108 | The rexinoid LG100754 is a novel RXR:PPARgamma agonist and decreases glucose levels in vivo. Mol Endocrinol. 2001 Aug;15(8):1360-9. | ||||
Ref 526251 | Co-regulator recruitment and the mechanism of retinoic acid receptor synergy. Nature. 2002 Jan 10;415(6868):187-92. | ||||
Ref 526387 | Novel retinoid X receptor antagonists: specific inhibition of retinoid synergism in RXR-RAR heterodimer actions. J Med Chem. 2002 Aug 1;45(16):3327-30. | ||||
Ref 527278 | Characterization of the interaction between retinoic acid receptor/retinoid X receptor (RAR/RXR) heterodimers and transcriptional coactivators through structural and fluorescence anisotropy studies. J Biol Chem. 2005 Jan 14;280(2):1625-33. Epub 2004 Nov 4. | ||||
Ref 527690 | J Med Chem. 2005 Aug 25;48(17):5383-403.Farnesoid X receptor: from structure to potential clinical applications. | ||||
Ref 533651 | Activation of mammalian retinoid X receptors by the insect growth regulator methoprene. Proc Natl Acad Sci U S A. 1995 Jun 20;92(13):6157-60. |
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