Large-scale Production and Protein Engineering of G Protein-coupled Receptors for Structural Studies

Overview

Journal Front Pharmacol

Date 2015 Apr 16

PMID 25873898

Citations 33

Authors

Dalibor Milic

Dmitry B Veprintsev

Affiliations

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Abstract

Structural studies of G protein-coupled receptors (GPCRs) gave insights into molecular mechanisms of their action and contributed significantly to molecular pharmacology. This is primarily due to technical advances in protein engineering, production and crystallization of these important receptor targets. On the other hand, NMR spectroscopy of GPCRs, which can provide information about their dynamics, still remains challenging due to difficulties in preparation of isotopically labeled receptors and their low long-term stabilities. In this review, we discuss methods used for expression and purification of GPCRs for crystallographic and NMR studies. We also summarize protein engineering methods that played a crucial role in obtaining GPCR crystal structures.

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