Number of the records: 1
Allosteric Modulation of GPCRs of Class A by Cholesterol
- 1.
SYSNO ASEP 0541423 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Allosteric Modulation of GPCRs of Class A by Cholesterol Author(s) Jakubík, Jan (FGU-C) RID, ORCID
El-Fakahany, E. E. (US)Article number 1953 Source Title International Journal of Molecular Sciences. - : MDPI
Roč. 22, č. 4 (2021)Number of pages 18 s. Language eng - English Country CH - Switzerland Keywords GPCRs ; cholesterol ; allosteric modulation Subject RIV ED - Physiology OECD category Physiology (including cytology) R&D Projects GA19-05318S GA ČR - Czech Science Foundation (CSF) Method of publishing Open access Institutional support FGU-C - RVO:67985823 UT WOS 000623814100001 EID SCOPUS 85101171435 DOI 10.3390/ijms22041953 Annotation 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. Workplace Institute of Physiology Contact Lucie Trajhanová, lucie.trajhanova@fgu.cas.cz, Tel.: 241 062 400 Year of Publishing 2022 Electronic address https://www.mdpi.com/1422-0067/22/4/1953
Number of the records: 1