Faculty Collaboration Database

Successful Strategies to Determine High-Resolution Structures of GPCRs. Trends Pharmacol Sci 2016 Dec;37(12):1055-1069

Date

10/12/2016

Pubmed ID

27726881

DOI

10.1016/j.tips.2016.09.009

Scopus ID

2-s2.0-84992170625 (requires institutional sign-in at Scopus site)   60 Citations

Abstract

G protein-coupled receptors (GPCRs) constitute the largest class of drug targets in the human genome, which highlights the importance of understanding the molecular basis of their activation, downstream signaling, and regulation. Since 2007, great progress has been made in the field of GPCR structure determination and their signaling complexes at the molecular level. Here, we summarize the high-resolution structures of over 30 different GPCRs with their co-crystallized ligands, and outline the successful strategies involved, including construct design, expression systems, and lipidic cubic phase (LCP) composition, and the many key technical parameters of the crystallization methods. By comparing the success rates of different strategies used in the past, we wish to pave the road for more successful structure-function research for GPCRs in the future.

Author List

Xiang J, Chun E, Liu C, Jing L, Al-Sahouri Z, Zhu L, Liu W

Authors

Wei Liu PhD Professor in the Pharmacology and Toxicology department at Medical College of Wisconsin
Lan Zhu PhD Assistant Professor in the Pharmacology and Toxicology department at Medical College of Wisconsin

MESH terms used to index this publication - Major topics in bold

Animals
Crystallization
Genome, Human
Humans
Ligands
Lipids
Protein Conformation
Protein Engineering
Receptors, G-Protein-Coupled
Signal Transduction