Litcius/Paper detail

Allosteric Modulation of Muscarinic Receptors by Cholesterol, Neurosteroids and Neuroactive Steroids

Ewa Szczurowska, Eszter Szánti‐Pintér, Alena Randáková, Ján Jakubík, Eva Kudová

2022International Journal of Molecular Sciences19 citationsDOIOpen Access PDF

Abstract

Muscarinic acetylcholine receptors are membrane receptors involved in many physiological processes. Malfunction of muscarinic signaling is a cause of various internal diseases, as well as psychiatric and neurologic conditions. Cholesterol, neurosteroids, neuroactive steroids, and steroid hormones are molecules of steroid origin that, besides having well-known genomic effects, also modulate membrane proteins including muscarinic acetylcholine receptors. Here, we review current knowledge on the allosteric modulation of muscarinic receptors by these steroids. We give a perspective on the research on the non-genomic effects of steroidal compounds on muscarinic receptors and drug development, with an aim to ultimately exploit such knowledge.

Topics & Concepts

Neuroactive steroidMuscarinic acetylcholine receptorMuscarinic acetylcholine receptor M4Muscarinic acetylcholine receptor M5Allosteric regulationMuscarinic acetylcholine receptor M3ReceptorMuscarinic acetylcholine receptor M1ChemistryMuscarinic acetylcholine receptor M2PharmacologyBiochemistryBiologyGABAA receptorReceptor Mechanisms and SignalingNeuroscience and Neuropharmacology ResearchLipid Membrane Structure and Behavior