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Updated: Jul 6, 2025

Quantifying Agonist Activity at G Protein-coupled Receptors
Published on: December 26, 2011
Dynamics of receptor activation by agonists
1Department of Physiology and Biophysics, State University of New York at Buffalo, Buffalo, New York.
Abstract:
How do agonists turn on receptors? The model system we have used to address this question is the adult-type skeletal muscle nicotinic acetylcholine receptor. This ligand-gated ion channel has two orthosteric sites (for neurotransmitters) in the extracellular domain linked to an allosteric site (a gate) in the transmembrane domain. The goal of this perspective is to summarize how measurements of agonist binding energy reveal the dynamics of the neurotransmitter sites and the fundamental link between binding and gating.
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