Peptide and trace amine orphan receptors: prospects for new therapeutic targets.
Over 20 orphan receptors predicted to exist from the human genome have now been paired with their cognate peptide ligand. In human tissues, expression of mRNA encoding several of these peptides (including bovine adrenomedullary peptide, orexins, prolactin-releasing peptide, tuberoinfundibular peptide 39 and neuropeptide B and W) and their receptors is predominantly in the CNS, implying a central role. However, ligand-binding and functional studies suggest that urotensin II, apelin, ghrelin, relaxin and urocortins, together with the trace amine tyramine, may have a role in the human cardiovascular system, with the prospect of becoming new therapeutic targets.
Davenport
Anthony P
AP
Clinical Pharmacology Unit, University of Cambridge, Level 6, Centre for Clinical Investigation, Addenbrooke's Hospital, Cambridge, CB2 2QQ, UK. apd10@medschl.cam.ac.uk
D000818:Animals; D001679:Biogenic Amines / Q000819:agonists / Q000037:antagonists & inhibitors / Q000502:physiology*; D016503:Drug Delivery Systems / Q000379:methods*; D006801:Humans; D018000:Receptors, Peptide / Q000819:agonists / Q000037:antagonists & inhibitors / Q000502:physiology*; D014661:Vasoconstriction / Q000187:drug effects / Q000502:physiology; D014664:Vasodilation / Q000187:drug effects / Q000502:physiology
D001679:Biogenic Amines; D018000:Receptors, Peptide