General Information of the Protein
Protein ID
PT01621
Protein Name
Retinoic acid receptor alpha
Secondarily
Protein Name
Nuclear receptor subfamily 1 group B member 1
Gene Name
RARA
Secondarily
Gene Name
Nr1b1
Sequence
MASNSSSCPTPGGGHLNGYPVPPYAFFFPPMLGGLSPPGALTSLQHQLPVSGYSTPSPATIETQSSSSEEIVPSPPSPPPLPRIYKPCFVCQDKSSGYHYGVSACEGCKGFFRRSIQKNMVYTCHRDKNCIINKVTRNRCQYCRLQKCFDVGMSKESVRNDRNKKKKEAPKPECSESYTLTPEVGELIEKVRKAHQETFPALCQLGKYTTNNSSEQRVSLDIDLWDKFSELSTKCIIKTVEFAKQLPGFTTLTIADQITLLKAACLDILILRICTRYTPEQDTMTFSDGLTLNRTQMHNAGFGPLTDLVFAFANQLLPLEMDDAETGLLSAICLICGDRQDLEQPDKVDMLQEPLLEALKVYVRKRRPSRPHMFPKMLMKITDLRSISAKGAERVITLKMEIPGSMPPLIQEMLENSEGLDTLSGQSGGGTRDGGGLAPPPGSCSPSLSPSSHRSSPATQSP
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Organism
Mus musculus, Mouse
Protein Classification
Transcription factor
>
Nuclear receptor
>
Nuclear hormone receptor subfamily 1
>
Nuclear hormone receptor subfamily 1 group B
>
Nuclear hormone receptor subfamily 1 group B member 1
Function
Receptor for retinoic acid (PubMed:17205979). 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 (PubMed:17205979). The RXR/RAR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5 (PubMed:17205979). 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 associate with the coactivators leading to transcriptional activation (PubMed:17205979, PubMed:9230306, PubMed:19078967). Formation of heterocomplex with histone deacetylases might lead to inhibition of RARE DNA element binding and to transcriptional repression (By similarity). Transcriptional activation and RARE DNA element binding might be supported by the transcription factor KLF2 (By similarity). RARA plays an essential role in the regulation of retinoic acid-induced germ cell development during spermatogenesis (PubMed:15901285). Has a role in the survival of early spermatocytes at the beginning prophase of meiosis (PubMed:15901285, PubMed:17905941). In Sertoli cells, may promote the survival and development of early meiotic prophase spermatocytes (PubMed:10660575, PubMed:17905941). In concert with RARG, required for skeletal growth, matrix homeostasis and growth plate function (PubMed:19389355). Together with RXRA, positively regulates microRNA-10a expression, thereby inhibiting the GATA6/VCAM1 signaling response to pulsatile shear stress in vascular endothelial cells (By similarity). In association with HDAC3, HDAC5 and HDAC7 corepressors, plays a role in the repression of microRNA-10a and thereby promotes the inflammatory response (By similarity).
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Uniprot ID
Primary ID:
P11416

Secondarily ID:
P22603
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Subcellular Location
Nucleus
Cytoplasm
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 = 18 nM
   TI
   LI
   LO
   TS
CP0040160
9-cis-retinoic acid (9cRA)
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C20H28O2
 1
1
EC50 = 22 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 = 33 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 = 51 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 > 1000 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 > 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
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
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0040160
9-cis-retinoic acid (9cRA)
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C20H28O2
 3
1 IC50 = 5 nM
2 IC50 = 6 nM
3 Kd = 15 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 = 11 nM
2 IC50 = 14 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 = 31 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 = 35 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 = 900 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 > 1000 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 > 1000 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 > 2000 nM
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT01452 Retinoic acid receptor beta Homo sapiens, Human
PT01475 Retinoic acid receptor alpha Homo sapiens, Human