Title: Agonist efficiency and a zipper mechanism for receptor conformational change.
Speaker: Anthony Auerbach, Professor, Department of Physiology and Biophysics, Jacobs School of Medicine & Biomedical Sciences, The State University of New York at Buffalo, Buffalo, New York
Dr. Auerbach's team use kinetics to probe events that comprise the binding and gating reactions of nicotinic acetylcholine receptors. Efficiency is a newly defined agonist property that is the percent of binding energy converted into energy for receptor activation. Efficiency is the correlation between affinity and efficacy and pertains to all agonists and receptors. Agonists belong to discrete efficiency classes with values that depend on agonist and binding site structures. The existence of efficiency classes indicates that ligand binding and receptor activation are not independent processes but rather are joined to form a single reaction coordinate. In the zipper mechanism for receptor conformational change, domains rearrange in sequence by progressing through a chain of linear free energy relationships.
