G-PROTEIN-COUPLED RECEPTORS IN SACCHAROMYCES-CEREVISIAE - HIGH-THROUGHPUT SCREENING ASSAYS FOR DRUG DISCOVERY

G-protein-coupled receptors are an important class of therapeutic drug targets by virtue of their roles in the regulation of diverse cellula r functions. Recent advances in the expression of heterologous G-prote in-coupled receptors in the yeast Saccharomyces cerevisiae have led to the development of sensitive and selective assays of their ligand-ind uced activation. Implementation of this new technology in the high-thr oughput screening of compound libraries has enabled the discovery of n ovel ligands for the G-protein-coupled somatostatin receptor. This art icle describes the broad applicability of the technology and its use i n drug discovery.