Journal
PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS
Volume 90, Issue 10, Pages 1779-1785Publisher
WILEY
DOI: 10.1002/prot.26302
Keywords
ATP; channels; receptors; structural biology
Categories
Funding
- Ministry of Science and Technology of the People's Republic of China [2016YFA0502800]
- National Natural Science Foundation of China [32071234]
- Open Research Fund of State Key Laboratory of Genetic Engineering, Fudan University [SKLGE-2105]
- Education Commission of Shanghai Municipality [ZDSYS14005]
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This review article discusses recent progress in understanding the structures and mechanisms of P2X receptors, particularly focusing on ATP binding and conformational changes during the gating cycle. It also provides a summary of the binding sites and regulatory mechanisms of various antagonists for P2X receptors.
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.
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