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Open AccessFeature PaperReview

Current Advances in Allosteric Modulation of Muscarinic Receptors

1
Department of Neurochemistry, Institute of Physiology CAS, 142 20 Prague, Czech Republic
2
Department of Experimental and Clinical Pharmacology, University of Minnesota College of Pharmacy, Minneapolis, MN 55455, USA
*
Authors to whom correspondence should be addressed.
Biomolecules 2020, 10(2), 325; https://doi.org/10.3390/biom10020325
Received: 17 January 2020 / Revised: 14 February 2020 / Accepted: 16 February 2020 / Published: 18 February 2020
Allosteric modulators are ligands that bind to a site on the receptor that is spatially separated from the orthosteric binding site for the endogenous neurotransmitter. Allosteric modulators modulate the binding affinity, potency, and efficacy of orthosteric ligands. Muscarinic acetylcholine receptors are prototypical allosterically-modulated G-protein-coupled receptors. They are a potential therapeutic target for the treatment of psychiatric, neurologic, and internal diseases like schizophrenia, Alzheimer’s disease, Huntington disease, type 2 diabetes, or chronic pulmonary obstruction. Here, we reviewed the progress made during the last decade in our understanding of their mechanisms of binding, allosteric modulation, and in vivo actions in order to understand the translational impact of studying this important class of pharmacological agents. We overviewed newly developed allosteric modulators of muscarinic receptors as well as new spin-off ideas like bitopic ligands combining allosteric and orthosteric moieties and photo-switchable ligands based on bitopic agents. View Full-Text
Keywords: acetylcholine; muscarinic receptors; allosteric modulation acetylcholine; muscarinic receptors; allosteric modulation
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Jakubik, J.; El-Fakahany, E.E. Current Advances in Allosteric Modulation of Muscarinic Receptors. Biomolecules 2020, 10, 325.

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