Alcohol-binding sites in distinct brain proteins: the quest for atomic level resolution.

ABSTRACT: Defining the sites of action of ethanol on brain proteins is a major prerequisite to understanding the molecular pharmacology of this drug. The main barrier to reaching an atomic-level understanding of alcohol action is the low potency of alcohols, ethanol in particular, which is a reflection of transient, low-affinity interactions with their targets. These mechanisms are difficult or impossible to study with traditional techniques such as radioligand binding or spectroscopy. However, there has been considerable recent progress in combining X-ray crystallography, structural modeling, and site-directed mutagenesis to define the sites and mechanisms of action of ethanol and related alcohols on key brain proteins. We review such insights for several diverse classes of proteins including inwar

SUBMITTER: Howard RJ 

PROVIDER: S-EPMC3201783 | biostudies-literature | 2011 Sep

REPOSITORIES: biostudies-literature