Počet záznamů: 1
Allosteric Modulation of GPCRs of Class A by Cholesterol
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SYSNO ASEP 0541423 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Allosteric Modulation of GPCRs of Class A by Cholesterol Tvůrce(i) Jakubík, Jan (FGU-C) RID, ORCID
El-Fakahany, E. E. (US)Číslo článku 1953 Zdroj.dok. International Journal of Molecular Sciences. - : MDPI
Roč. 22, č. 4 (2021)Poč.str. 18 s. Jazyk dok. eng - angličtina Země vyd. CH - Švýcarsko Klíč. slova GPCRs ; cholesterol ; allosteric modulation Vědní obor RIV ED - Fyziologie Obor OECD Physiology (including cytology) CEP GA19-05318S GA ČR - Grantová agentura ČR Způsob publikování Open access Institucionální podpora FGU-C - RVO:67985823 UT WOS 000623814100001 EID SCOPUS 85101171435 DOI 10.3390/ijms22041953 Anotace 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. Pracoviště Fyziologický ústav Kontakt Lucie Trajhanová, lucie.trajhanova@fgu.cas.cz, Tel.: 241 062 400 Rok sběru 2022 Elektronická adresa https://www.mdpi.com/1422-0067/22/4/1953
Počet záznamů: 1