Dynamics of receptor activation by agonists

Biophys J. 2024 Jan 4:S0006-3495(24)00003-1. doi: 10.1016/j.bpj.2024.01.003. Online ahead of print.ABSTRACTHow do agonists turn on receptors? The model system we have used to address this question is the adult-type skeletal muscle nicotinic acetylcholine receptor (AChR). This ligand-gated ion channel has 2 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.PMID:38178577 | DOI:10.1016/j.bpj.2024.01.003

Source: Biophysical Journal - January 5, 2024 Category: Physics Authors: Anthony Auerbach Source Type: research