Chapter 30. Progress in the Characterization of Peptide Receptors

Abstract

Publisher Summary This chapter discusses the selected recent research on receptors for peptides of medicinal interest, focusing mainly on G protein-coupled receptors and growth factor receptors/tyrosine kinases. Recombinant DNA technology has been a ground-breaking tool in these efforts. In general, regardless of the structural class, receptor functions, such as ligand binding, signal transduction, and receptor internalization (regulation) are carried out independently by separate domains of a single chain or by different receptor subunits or accessory proteins. It has been more difficult to characterize the complete second messenger cascade triggered by ligand-receptor binding, partly because many of the ligands mediate a plethora of effects; an interesting new development is the involvement of G-proteins and phosphoinositides with many of the growth factor receptors. Protein and cellular biochemistry are coming to the fore in solving these problems now that molecular genetics has provided much of the necessary information on receptor structure. Another development likely to advance the understanding of the receptor structure and function is the continued discovery of nonpeptide receptor antagonists. Such molecules have already provided the basis for important contributions in the cholecystokinin (CCK) and all areas. New antagonists for the LH-RH receptor, and presumably for other receptors as well, are likely to serve to accelerate the pace of discovery in the field of receptor structure and function.