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. 2018:603:21-47.
doi: 10.1016/bs.mie.2018.01.017. Epub 2018 Mar 24.

X-Ray Crystallographic Studies for Revealing Binding Sites of General Anesthetics in Pentameric Ligand-Gated Ion Channels

Qiang Chen  1 , Yan Xu  1 , Pei Tang  2
Affiliations

X-Ray Crystallographic Studies for Revealing Binding Sites of General Anesthetics in Pentameric Ligand-Gated Ion Channels

Qiang Chen et al. Methods Enzymol. 2018.

Abstract

X-ray crystallography is a powerful tool in structural biology and can offer insight into structured-based understanding of general anesthetic action on various relevant molecular targets, including pentameric ligand-gated ion channels (pLGICs). In this chapter, we outline the procedures for expression and purification of pLGICs. Optimization of crystallization conditions, especially to achieve high-resolution structures of pLGICs bound with general anesthetics, is also presented. Case studies of pLGICs bound with the volatile general anesthetic isoflurane, 2-bromoethanol, and the intravenous general anesthetic ketamine are revisited.

Keywords: General anesthetics; X-ray crystallography; pLGICs.

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