Corticotropin-Releasing Factor Receptor 1 Antibodies
The human CRF1 receptor is widely expressed in the central nervous system with high levels of expression in cortex, cerebellum, hippocampus, basolateral amygdala, bed nucleus of the stria terminalis, olfactory bulb and anterior pituitary. In the periphery, CRF1 receptor is expressed at low levels in the skin, ovary, testis and adrenal gland. CRF, urocortin 1 (UCN1) and urotensin I all bind with high affinity to the mammalian CRF1 receptor and activate the cyclic AMP signaling pathway. In contrast, UCN2 and UCN3 do not bind to or activate CRF1 receptors. Therefore, CRF and urocortin 1 can be classified as the endogenous ligands for mammalian CRF1 receptors. CRF1 receptor desensitization, β-arrestin recruitment and internalization are regulated by phosphorylation of carboxyl-terminal threonine428/serine429 (pT428/pS429-CRF1), threonine431/serine434 (pT431/pS434-CRF1) and serine437/serine441 (pS437/pS441-CRF1). This nomenclature refers to the human CRF1 receptor. This phosphorylation motif is highly conserved across species but corresponds to pT399/pS400-CRF1, pT402/pS405-CRF1 and pS408/pS412-CRF1 in mice and rats. Interestingly, a very similar phosphorylation motif is present in the human CRF2 receptor which corresponds to pT395/pS396-CRF2, pT398/pS401-CRF2 and pS404/pT408-CRF2. For more information on CRF1 pharmacology please refer to the IUPHAR database. For further reading refer to:
Hauger RL, Grigoriadis DE, Dallman MF, Plotsky PM, Vale WW, Dautzenberg FM. International Union of Pharmacology. XXXVI. Current status of the nomenclature for receptors for corticotropin-releasing factor and their ligands. Pharmacol Rev. 2003 Mar;55(1):21-6. doi: 10.1124/pr.55.1.3. PMID: 12615952.