hide
Free keywords:
Binding-site stereochemistry, ionotropic glutamate
receptors, ionotropic glutamate receptor activation, ligandgated
ion channels, protein conformational changes,
thermodynamics
Abstract:
As with all ligand-gated ion channels, ionotropic glutamate receptors (iGluRs) convert the free energy of agonist-binding into a sequence of conformational changes that allow regulated ion flux across an otherwise insulating membrane bilayer. In the case of iGluRs, the resulting membrane depolarization is a key mediator of intercellular signals in the synapses of the CNS. Recent biomedical and structural research has greatly expanded our understanding of the chemistry of iGluR agonist binding, and of the subsequent molecular changes that drive channel gating and desensitization.
