“Structure of the Pentameric Ligand-Gated Ion Channel ELIC Cocrystallized With its Competitive Antagonist Acetylcholine,” authored by Jianjun Pan, Qiang Chen, Dan Willenbring, Ken Yoshida, Tommy Tillman, Ossama B. Kashlan, Aina Cohen, Xiang-Peng Kong, Yan Xu, and Pei Tang, was recently published in the online journal Nature Communications (2012;3:714). The group’s work was also selected as the March 6 issue’s featured image.
In their paper, the authors show that acetylcholine is a competitive antagonist for ELIC, the pentameric ligand-gated ion channel from the bacteria Erwinia chrysanthemi. ELIC is a prototype for Cys-loop receptors, which mediate fast chemical to electrical transduction throughout the nervous system and are important therapeutic targets for many diseases. Their work presents a compelling case for understanding the structural underpinning of the functional relationship between agonism and competitive antagonism in the Cys-loop receptors, providing a new framework for developing novel therapeutic drugs.