Abstract

G-protein coupled receptors (GPCRs) are proteins of the plasma membrane, which are characterized by seven membrane-spanning segments (TMs). GPCRs play an important role in almost all of our physiological and pathophysiological conditions by interacting with a large variety of ligands and stimulating different G-proteins and signaling cascades. By playing a key role in the function of our body and being involved in the pathophysiology of many disorders, GPCRs are very important therapeutic targets. Determination of the structure and function of GPCRs could advance the design of novel receptor-specific drugs against various diseases. A powerful method to obtain structural and functional information for GPCRs is the cysteine substituted accessibility method (SCAM). SCAM is used to systematically map the TM residues of GPCRs and determine their functional role. SCAM can also be used to determine differences in the structures of the TMs in different functional states of GPCRs.

Keywords: Binding-site crevice, cysteine substituted accessibility method, function, G-protein coupled receptors, methanothiosulfonate reagents, structure.