aryl hydrocarbon receptor; Ah receptor; AhR; dioxin receptor (AHR)
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Function
- ligand-activated transcriptional activator
- role in cell-cycle regulation
- likely to play a role in the development & maturation of many tissues
- binds to DNA as heterodimer with ARNT (Ah receptor complex)
- efficient DNA binding requires dimerization with another bHLH protein
- in the nucleus, heterodimer of AHR & ARNT
- interacts with coactivators including SRC-1, RIP140 & NOCA7, & with the corepressor SMRT
- interacts with NEDD8 & IVNS1ABP
- binds MYBBP1A (putative)
- interacts with HSP90
Structure
- contains 1 basic helix-loop-helix (bHLH) domain
- contains 1 PAC domain (PAS-associated C-terminal domain)
- contains 2 PAS domains (PER-ARNT-SIM domains)
Compartment
- cytoplasm. nucleus
- first cytoplasmic
- upon binding with ligand & interaction with a HSP90, it translocates to the nucleus
Expression
- expressed in all tissues tested, including blood, brain, heart, kidney, liver, lung, pancreas & skeletal muscle
- induced or repressed by TGF-beta & dioxin (cell-type specific)
- repressed by cAMP, retinoic acid, & TPA
Pharmacology
- aryl hydrocarbon receptor antagonists promote the expansion of human hematopoietic stem cells
More general terms
Additional terms
- 2,3,7,8-tetrachlorodibenzo-p-dioxin (dioxin TCDD)
- AH receptor-interacting protein; AIP; aryl-hydrocarbon receptor-interacting protein; immunophilin homolog ARA9; HBV X-associated protein 2; XAP-2 (AIP, XAP2)
- aryl hydrocarbon [Ah] receptor complex
References
- ↑ Hoffman EC et al Cloning of a factor required for activity of the Ah (dioxin) receptor. Science. 1991 May 17;252(5008):954-8. PMID: https://www.ncbi.nlm.nih.gov/pubmed/1852076
- ↑ UniProt http://www.uniprot.org/uniprot/P35869.html
- ↑ Boitano AE et al. Aryl hydrocarbon receptor antagonists promote the expansion of human hematopoietic stem cells. Science 2010 Sep 10; 329:1345 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/20688981 <Internet> http://dx.doi.org/10.1126/science.1191536
Sauvageau G and Humphries RK. The blood stem cell Holy Grail? Science 2010 Sep 10; 329:1291. <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/20829472 <Internet> http://dx.doi.org/10.1126/science.1195173