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Updated: Aug 16, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
[Allosteric regulation of receptors. I. Cooperative interaction and functional regulation]
Abstract:
Today thousands of scientific publications in the field of receptology are dedicated to allosteric regulation of receptors. Biochemical events in cardiovascular, nerve, immune, endocrine, and other systems are based on various allosteric processes. Many of pharmaceuticals exert their action via allosteric regulation of receptive structures. Unfortunately, original publications sometimes are rather fragmentary. The history, methodology, classification as well as functional aspects of allosteric regulation of receptors are reviewed in the present paper. On the basis of topography of orthosteric and allosteric receptor binding sites allosteric regulation may be subdivided into: specific, non-specific, functional, and cooperative interaction. The results of allosteric regulation of receptors by metal cations are summarized. Agonists and antagonists receptor interaction are described from the point of view of allosteric regulation.
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