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Pharmacology of Free Fatty Acid Receptors and Their Allosteric Modulators

Allosteric Modulation of GPCRs of Class A by Cholesterol

Department of Neurochemistry, Institute of Physiology Czech Academy of Sciences, 142 20 Prague, Czech Republic
Department of Experimental and Clinical Pharmacology, University of Minnesota College of Pharmacy, Minneapolis, MN 55455, USA
Authors to whom correspondence should be addressed.
Academic Editor: Alexander O. Shpakov
Int. J. Mol. Sci. 2021, 22(4), 1953;
Received: 20 January 2021 / Revised: 11 February 2021 / Accepted: 12 February 2021 / Published: 16 February 2021
(This article belongs to the Special Issue Allosteric Modulators of GPCRs)
G-protein coupled receptors (GPCRs) are membrane proteins that convey extracellular signals to the cellular milieu. They represent a target for more than 30% of currently marketed drugs. Here we review the effects of membrane cholesterol on the function of GPCRs of Class A. We review both the specific effects of cholesterol mediated via its direct high-affinity binding to the receptor and non-specific effects mediated by cholesterol-induced changes in the properties of the membrane. Cholesterol binds to many GPCRs at both canonical and non-canonical binding sites. It allosterically affects ligand binding to and activation of GPCRs. Additionally, it changes the oligomerization state of GPCRs. In this review, we consider a perspective of the potential for the development of new therapies that are targeted at manipulating the level of membrane cholesterol or modulating cholesterol binding sites on to GPCRs. View Full-Text
Keywords: GPCRs; cholesterol; allosteric modulation GPCRs; cholesterol; allosteric modulation
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MDPI and ACS Style

Jakubík, J.; El-Fakahany, E.E. Allosteric Modulation of GPCRs of Class A by Cholesterol. Int. J. Mol. Sci. 2021, 22, 1953.

AMA Style

Jakubík J, El-Fakahany EE. Allosteric Modulation of GPCRs of Class A by Cholesterol. International Journal of Molecular Sciences. 2021; 22(4):1953.

Chicago/Turabian Style

Jakubík, Jan, and Esam E. El-Fakahany 2021. "Allosteric Modulation of GPCRs of Class A by Cholesterol" International Journal of Molecular Sciences 22, no. 4: 1953.

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