Recent progress in the structural biology of P2X receptors.
ATP
channels
receptors
structural biology
Journal
Proteins
ISSN: 1097-0134
Titre abrégé: Proteins
Pays: United States
ID NLM: 8700181
Informations de publication
Date de publication:
10 2022
10 2022
Historique:
revised:
04
01
2022
received:
24
09
2021
accepted:
11
01
2022
pubmed:
14
1
2022
medline:
28
9
2022
entrez:
13
1
2022
Statut:
ppublish
Résumé
P2X receptors are ATP-gated trimeric nonselective cation channels that are important for various physiological and pathological processes, including synaptic transmission, pain perception, immune regulation, and apoptosis. Accordingly, they attract a wide range of interest as drug targets, such as those for chronic cough, neuropathic pain, and depression. After the zebrafish P2X4 receptor structure was reported in 2009, various other P2X receptor structures have been reported, extending our understanding of the molecular mechanisms of P2X receptors. This review article describes the recent progress on understanding the structures and mechanisms of P2X receptors, especially of the mechanisms underlying ATP binding and conformational changes during the gating cycle. In addition, since several antagonists for different P2X subtypes have entered into clinical trials, this review also summarizes the binding sites and regulatory mechanisms of these antagonists, which may contribute to new strategies of targeting P2X receptors for drug discovery.
Substances chimiques
Receptors, Purinergic P2X
0
Receptors, Purinergic P2X4
0
Adenosine Triphosphate
8L70Q75FXE
Types de publication
Journal Article
Review
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
1779-1785Informations de copyright
© 2022 Wiley Periodicals LLC.
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