Evidence for Free Radical Drug Ligands in class A G-protein Coupled Receptors

Abstract

AbstractWe analyse the conformation of 22 cationic ligands bound to G-protein coupled receptors of known structure and find three ligands that are present inside receptors not in their closed shell cation form, but as neutral radicals, i.e. after addition of an electron to the ligand. The implications of this finding for GPCR function are discussed and a possible experimental test is proposed.