CRHR1
Description
The CRHR1 (corticotropin releasing hormone receptor 1) is a protein-coding gene located on chromosome 17.
CRHR1, also known as CRF1, is a protein encoded by the CRHR1 gene located at region 17q21.31 on the human chromosome. It is composed of 444 amino acids and contains 14 exons spanning 20 kb of DNA. The primary functional CRF1 isoform, containing 415 amino acids, arises from the excision of exon 6. This isoform is structured with seven hydrophobic alpha-helices. The CRHR1 gene undergoes alternative splicing, producing variants through deletion of exons. These variants, though not identified in native tissues, suggest the presence of alternate CRF receptors with differing binding capabilities and signaling mechanisms. CRHR1 shares 70% homology with CRF2, another human CRF receptor family, with the most significant divergence observed at the N-terminus. CRF1 is activated by the binding of CRF or a CRF-agonist.
CRHR1 acts as a G-protein coupled receptor for both corticotropin-releasing factor (CRH) and urocortin (UCN). It exhibits high affinity for these ligands, and upon binding, undergoes a conformational change that initiates signaling through guanine nucleotide-binding proteins (G proteins) and downstream effectors, including adenylate cyclase. This activation leads to increased intracellular cAMP levels. Additionally, CRHR1 inhibits the activity of the calcium channel CACNA1H. CRHR1 is essential for normal embryonic development of the adrenal gland and for proper hormonal responses to stress. It also plays a crucial role in mediating responses to anxiogenic stimuli.
CRHR1 is also known as CRF-R, CRF-R-1, CRF-R1, CRF1, CRFR-1, CRFR1, CRH-R-1, CRH-R1, CRHR, CRHR1L.
