General Information of the Protein
Protein ID
PT03152
Protein Name
Retinoic acid receptor RXR-alpha
Secondarily
Protein Name
Nuclear receptor subfamily 2 group B member 1
Retinoid X receptor alpha
Gene Name
RXRA
Secondarily
Gene Name
Nr2b1
Sequence
MDTKHFLPLDFSTQVNSSSLNSPTGRGSMAVPSLHPSLGPGIGSPLGSPGQLHSPISTLSSPINGMGPPFSVISSPMGPHSMSVPTTPTLGFGTGSPQLNSPMNPVSSTEDIKPPLGLNGVLKVPAHPSGNMASFTKHICAICGDRSSGKHYGVYSCEGCKGFFKRTVRKDLTYTCRDNKDCLIDKRQRNRCQYCRYQKCLAMGMKREAVQEERQRGKDRNENEVESTSSANEDMPVEKILEAELAVEPKTETYVEANMGLNPSSPNDPVTNICQAADKQLFTLVEWAKRIPHFSELPLDDQVILLRAGWNELLIASFSHRSIAVKDGILLATGLHVHRNSAHSAGVGAIFDRVLTELVSKMRDMQMDKTELGCLRAIVLFNPDSKGLSNPAEVEALREKVYASLEAYCKHKYPEQPGRFAKLLLRLPALRSIGLKCLEHLFFFKLIGDTPIDTFLMEMLEAPHQAT
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Organism
Mus musculus, Mouse
Protein Classification
Transcription factor
>
Nuclear receptor
>
Nuclear hormone receptor subfamily 2
>
Nuclear hormone receptor subfamily 2 group B
>
Nuclear hormone receptor subfamily 2 group B member 1
Function
Receptor for retinoic acid that acts as a transcription factor (PubMed:10383391, PubMed:12032153, PubMed:25417649). Forms homo- or heterodimers with retinoic acid receptors (RARs) and binds to target response elements in response to their ligands, all-trans or 9-cis retinoic acid, to regulate gene expression in various biological processes (PubMed:1310259, PubMed:10383391). The RAR/RXR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5 to regulate transcription (PubMed:1310259). The high affinity ligand for retinoid X receptors (RXRs) is 9-cis retinoic acid (PubMed:10383391, PubMed:25417649). In the absence of ligand, the RXR-RAR heterodimers associate with a multiprotein complex containing transcription corepressors that induce histone deacetylation, chromatin condensation and transcriptional suppression (By similarity). On ligand binding, the corepressors dissociate from the receptors and coactivators are recruited leading to transcriptional activation (By similarity). Serves as a common heterodimeric partner for a number of nuclear receptors, such as RARA, RARB and PPARA (PubMed:1310259). The RXRA/RARB heterodimer can act as a transcriptional repressor or transcriptional activator, depending on the RARE DNA element context (By similarity). The RXRA/PPARA heterodimer is required for PPARA transcriptional activity on fatty acid oxidation genes such as ACOX1 and the P450 system genes (By similarity). Together with RARA, positively regulates microRNA-10a expression, thereby inhibiting the GATA6/VCAM1 signaling response to pulsatile shear stress in vascular endothelial cells (By similarity). Acts as an enhancer of RARA binding to RARE DNA element (By similarity). May facilitate the nuclear import of heterodimerization partners such as VDR and NR4A1 (By similarity). Promotes myelin debris phagocytosis and remyelination by macrophages (PubMed:26463675). Plays a role in the attenuation of the innate immune system in response to viral infections, possibly by negatively regulating the transcription of antiviral genes such as type I IFN genes (PubMed:25417649). Involved in the regulation of calcium signaling by repressing ITPR2 gene expression, thereby controlling cellular senescence (By similarity).
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Uniprot ID
P28700
Ensembl ID
ENSG00000186350
Subcellular Location
Nucleus
Cytoplasm
Mitochondrion
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000044 , CV-1
Compound ID Compound Name Compound Formula
CP0126004
(2E,4E,6E,8Z)-3,7-Dimethyl-9-(2,6,6-trimethyl-cyclohex-1-enyl)-nona-2,4,6,8-tetraenoic acid
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C20H28O2
 1
1
EC50 = 27 nM
   TI
   LI
   LO
   TS
CP0004259
4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)vinyl]benzoic acid
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C24H28O2
 1
1
EC50 = 40 nM
   TI
   LI
   LO
   TS
CP0043939
(2E,4Z,6Z)-8-[3,4-Dihydro-2H-naphthalen-(1E)-ylidene]-3,7-dimethyl-octa-2,4,6-trienoic acid
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C20H22O2
 1
1
EC50 = 118 nM
   TI
   LI
   LO
   TS
CP0042977
9-cis retinoic acid
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C20H28O2
 1
1
EC50 = 200 nM
   TI
   LI
   LO
   TS
CP0082294
(2E,4Z,6Z)-8-[3-Ethyl-2-isopropyl-cyclohex-2-en-(E)-ylidene]-3,7-dimethyl-octa-2,4,6-trienoic acid
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C21H30O2
 1
1
EC50 = 220 nM
   TI
   LI
   LO
   TS
CP0153500
(E)-3-[5'-(Adamant-1-yl)-2-chloro-4'-hydroxy-2'-methylbiphenyl-4-yl]acrylic acid
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C26H27ClO3
 1
1
EC50 = 576 nM
   TI
   LI
   LO
   TS
CP0084055
(E)-3-[5'-(Adamant-1-yl)-2-chloro-4'-[(2-methoxyethoxy)methoxy]-2'-methylbiphenyl-4-yl]acrylic acid
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C30H35ClO5
 1
1
EC50 = 600 nM
   TI
   LI
   LO
   TS
CP0084902
6-[5-(Adamant-1-yl)-4-[(2-methoxyethoxy)methoxy]-2-methylphenyl]-5-chloro-2-naphthoic acid
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C32H35ClO5
 1
1
EC50 = 667 nM
   TI
   LI
   LO
   TS
CP0070442
2-[5'-(Adamant-1-yl)-2-chloro-4'-[(2-methoxyethoxy)methoxy]-2'-methylbiphenyl-4-yl]acetic Acid
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C29H35ClO5
 1
1
EC50 = 1137 nM
   TI
   LI
   LO
   TS
CP0040160
9-cis-retinoic acid (9cRA)
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C20H28O2
 1
1
EC50 > 2000 nM
   TI
   LI
   LO
   TS
CP0098128
(2E,4E,6E)-8-[3,4-Dihydro-2H-naphthalen-(1E)-ylidene]-3,7-dimethyl-octa-2,4,6-trienoic acid
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C20H22O2
 1
1
EC50 > 2000 nM
   TI
   LI
   LO
   TS
CP0101102
(2E,4E,6E)-8-[3-Ethyl-2-isopropyl-cyclohex-2-en-(E)-ylidene]-3,7-dimethyl-octa-2,4,6-trienoic acid
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C21H30O2
 1
1
EC50 > 2000 nM
   TI
   LI
   LO
   TS
CP0162300
(2Z,4E,6E)-8-[3,4-Dihydro-2H-naphthalen-(1E)-ylidene]-3,7-dimethyl-octa-2,4,6-trienoic acid
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C20H22O2
 1
1
EC50 > 2000 nM
   TI
   LI
   LO
   TS
CP0216905
(2Z,4E,6E)-8-[3-Ethyl-2-isopropyl-cyclohex-2-en-(E)-ylidene]-3,7-dimethyl-octa-2,4,6-trienoic acid
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C21H30O2
 1
1
EC50 > 2000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0042977
9-cis retinoic acid
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C20H28O2
 2
1 IC50 = 82 nM
2 Kd = 32 nM
CP0126004
(2E,4E,6E,8Z)-3,7-Dimethyl-9-(2,6,6-trimethyl-cyclohex-1-enyl)-nona-2,4,6,8-tetraenoic acid
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C20H28O2
 1
1 IC50 = 82 nM
CP0043939
(2E,4Z,6Z)-8-[3,4-Dihydro-2H-naphthalen-(1E)-ylidene]-3,7-dimethyl-octa-2,4,6-trienoic acid
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C20H22O2
 1
1 IC50 = 284 nM
CP0082294
(2E,4Z,6Z)-8-[3-Ethyl-2-isopropyl-cyclohex-2-en-(E)-ylidene]-3,7-dimethyl-octa-2,4,6-trienoic acid
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C21H30O2
 1
1 IC50 = 868 nM
CP0101102
(2E,4E,6E)-8-[3-Ethyl-2-isopropyl-cyclohex-2-en-(E)-ylidene]-3,7-dimethyl-octa-2,4,6-trienoic acid
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C21H30O2
 2
1 IC50 > 1000 nM
2 IC50 > 2000 nM
CP0216905
(2Z,4E,6E)-8-[3-Ethyl-2-isopropyl-cyclohex-2-en-(E)-ylidene]-3,7-dimethyl-octa-2,4,6-trienoic acid
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C21H30O2
 1
1 IC50 > 1000 nM
CP0040160
9-cis-retinoic acid (9cRA)
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C20H28O2
 3
1 IC50 > 2000 nM
2 IC50 > 50000 nM
3 Kd = 1000 nM
CP0098128
(2E,4E,6E)-8-[3,4-Dihydro-2H-naphthalen-(1E)-ylidene]-3,7-dimethyl-octa-2,4,6-trienoic acid
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C20H22O2
 1
1 IC50 > 2000 nM
CP0162300
(2Z,4E,6E)-8-[3,4-Dihydro-2H-naphthalen-(1E)-ylidene]-3,7-dimethyl-octa-2,4,6-trienoic acid
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C20H22O2
 1
1 IC50 > 2000 nM