Muscarinic Receptor: From Structure to Animal Models

0458562 - FGÚ 2017 RIV US eng M - Monography Chapter
Jakubík, Jan - El-Fakahany, E. E.
Allosteric Modulation of Muscarinic Receptors.
Muscarinic Receptor: From Structure to Animal Models. New York: Springer, 2016 - (Mysliveček, J.; Jakubík, J.), s. 95-130. Neuromethods, 107. ISBN 978-1-4939-2857-6
R&D Projects: GA ČR(CZ) GBP304/12/G069
Institutional support: RVO:67985823
Keywords : muscarinic receptors * allosteric modulation * radioligand binding functional response
Subject RIV: ED - Physiology

Allosteric ligands modulate binding and function of muscarinic receptors in a different way than orthosteric ligands. Unlike orthosteric ligands their effects are limited by a cooperativity factor. This imparts them unique properties, including cooperativity-based selectivity, functional selectivity and restoring of physiological-like space and time pattern of signaling under pathological conditions. Therefore, allosteric modulators of muscarinic receptor are intensively studied as possible therapeutics of pathological conditions including Alzheimer’s disease and schizophrenia. Research of allosteric modulation has pioneered the way for a whole class A of G-protein coupled receptors and has had an impact beyond its own field. We review principles of allosteric modulations and their implications for proper design of binding as well as functional experiments and for proper data analysis.
Permanent Link: http://hdl.handle.net/11104/0258820