STRUCTURE-FUNCTION RELATIONSHIP OF PROTEINS BELONGING TO THE FAMILY OF RECEPTORS COUPLED TO GTP-BINDING PROTEINS

The structural properties of a number of proteins belonging to the family of receptors coupled to GTP binding proteins are discussed in relation to their function. The structure of the ligand binding site and of the regions involved in coupling to the G proteins are analyzed mainly for the adrenergic and muscarinic cholinergic receptors, for which site-directed mutagenesis and chimaeric constructions have been studied. The structure of the genes are compared and the presence of various regulatory elements is discussed in relation to control of expression. Mechanism of desensitization and internalization, while mostly studied for the beta-2-adrenergic receptor, are proposed to be generally applicable to all G-protein-coupled receptors.