High-throughput screening assays for G-protein-coupled receptors-targeted drug discovery / 国际药学研究杂志

ABSTRACT

G-protein-coupled receptors (GPCR), also known as 7 trans-membrane receptors. are the largest family of cell surface receptois. GPCR mediate many important physiological functions and are among the most successful therapeutic targets for a broad spectrum of diseases. These receptors are the targets of >50% of the current therapeutic agents on the market. Therefore, GPCR assay development and GPCR ligand screening remain the major focus of drug discovery research worldwide. In this review. we summarize the most widely used GPCR assays and recent advances in high-throughput screening technology for GPCR drug discovery. © 2006 Editorial office of Foreign Medical Sciences.