Abstract

The number of G protein-coupled receptors (GPCRs) is growing daily, and more than 1000 genes have been cloned so far. Receptor-sequence analysis has divided GPCRs into three subfamilies: (1) rhodopsin or β-adrenoceptor-like; (2) secretin or glucagon-like receptors; and (3) metabotropic or chemosensor-like receptors. Peptide GPCRs are not structurally homogeneous as they belong to both class 1 [e.g. follicle-stimulating hormone (FSH), leutinizing hormone (LH) and neuropeptide Y receptors] and class 2 [e.g. vasoactive intestinal peptide (VIP), calcitonin and secretin receptors]. Peptide agonists that act through GPCRs can be small peptides such as enkephalins, bradykinin, substance P, calcitonin-gene-related peptide (CGRP) and VIP, large peptides or glycoproteins such as chemokines and hormones, or protease enzymes such as thrombin and trypsin. Given the heterogeneity of these receptors, the challenging aim of a recent course in Erice4Peptidergic G Protein-Coupled Receptors. From Basic Research to Clinical Applications, 14–24 May 1998, Erice, Italy.4 was to bring together a variety of approaches and to discuss recent advances in the field of GPCRs, ranging from basic research to clinical applications.

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