Structural Insights into Ligand Recognition and Selectivity for Classes A, B, and C GPCRs

Overview

Journal Eur J Pharmacol

Specialty Pharmacology

Date 2015 May 19

PMID 25981303

Citations 25

Authors

Sang-Min Lee

Jason M Booe

Augen A Pioszak

Affiliations

Soon will be listed here.

Abstract

The G protein-coupled receptor (GPCR) superfamily constitutes the largest collection of cell surface signaling proteins with approximately 800 members in the human genome. GPCRs regulate virtually all aspects of physiology and they are an important class of drug targets with ~30% of drugs on the market targeting a GPCR. Breakthroughs in GPCR structural biology in recent years have significantly expanded our understanding of GPCR structure and function and ushered in a new era of structure-based drug design for GPCRs. Crystal structures for nearly thirty distinct GPCRs are now available including receptors from each of the major classes, A, B, C, and F. These structures provide a foundation for understanding the molecular basis of GPCR pharmacology. Here, we review structural mechanisms of ligand recognition and selectivity of GPCRs with a focus on selected examples from classes A, B, and C, and we highlight major unresolved questions for future structural studies.

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