Allosteric Modulation of GPCRs of Class A by Cholesterol
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F67985823%3A_____%2F21%3A00541423" target="_blank" >RIV/67985823:_____/21:00541423 - isvavai.cz</a>
Result on the web
<a href="https://www.mdpi.com/1422-0067/22/4/1953" target="_blank" >https://www.mdpi.com/1422-0067/22/4/1953</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.3390/ijms22041953" target="_blank" >10.3390/ijms22041953</a>
Alternative languages
Result language
angličtina
Original language name
Allosteric Modulation of GPCRs of Class A by Cholesterol
Original language description
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.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
30105 - Physiology (including cytology)
Result continuities
Project
<a href="/en/project/GA19-05318S" target="_blank" >GA19-05318S: Molecular mechanisms of allosteric modulation of muscarinic acetylcholine receptors by neurosteroids and cholesterol</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)
Others
Publication year
2021
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
International Journal of Molecular Sciences
ISSN
1422-0067
e-ISSN
1422-0067
Volume of the periodical
22
Issue of the periodical within the volume
4
Country of publishing house
CH - SWITZERLAND
Number of pages
18
Pages from-to
1953
UT code for WoS article
000623814100001
EID of the result in the Scopus database
2-s2.0-85101171435