Common Anesthetic-binding Site for Inhibition of Pentameric Ligand-gated Ion Channels.

ABSTRACT:

Background

Identifying functionally relevant anesthetic-binding sites in pentameric ligand-gated ion channels (pLGICs) is an important step toward understanding the molecular mechanisms underlying anesthetic action. The anesthetic propofol is known to inhibit cation-conducting pLGICs, including a prokaryotic pLGIC from Erwinia chrysanthemi (ELIC), but the sites responsible for functional inhibition remain undetermined.

Methods

We photolabeled ELIC with a light-activated derivative of propofol (AziPm) and performed fluorine-19 nuclear magnetic resonance experiments to support propofol binding to a transmembrane domain (TMD) intrasubunit pocket. To differentiate sites responsible for propofol inhibition from those that are functionally irrelevant, we made an ELIC-γ-aminobutyri

SUBMITTER: Kinde MN 

PROVIDER: S-EPMC4755840 | biostudies-literature | 2016 Mar

REPOSITORIES: biostudies-literature