Mechanism of Allosteric Modulation of the Cys-loop Receptors.

ABSTRACT: The cys-loop receptor family is a major family of neurotransmitter-operated ion channels. They play important roles in fast synaptic transmission, controlling neuronal excitability, and brain function. These receptors are allosteric proteins, in that binding of a neurotransmitter to its binding site remotely controls the channel function. The cys-loop receptors also are subject to allosteric modulation by many pharmaceutical agents and endogenous modulators. By binding to a site of the receptor distinct from the neurotransmitter binding site, allosteric modulators alter the response of the receptors to their agonists. The mechanism of allosteric modulation is traditionally believed to be that allosteric modulators directly change the binding affinity of receptors for their agonists. More r

SUBMITTER: Chang Y 

PROVIDER: S-EPMC4033940 | biostudies-literature | 2010 Aug

REPOSITORIES: biostudies-literature