Journal
TRENDS IN BIOCHEMICAL SCIENCES
Volume 38, Issue 1, Pages 20-29Publisher
ELSEVIER SCIENCE LONDON
DOI: 10.1016/j.tibs.2012.10.006
Keywords
purinergic receptor; structure; ligand-gated ion channels; gating; neurotransmitter
Categories
Funding
- Centre National de la Recherche Scientifique
- Ministere de la Recherche
- International Center for Frontier Research in Chemistry
- Agence Nationale de la Recherche
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P2X receptors are nonselective cation channels gated by extracellular ATP. They represent new therapeutic targets, and they form channels with a unique trimeric architecture. In 2009, the first crystal structure of a P2X receptor was reported, in which the receptor was in an ATP-free, closed channel state. However, our view recently changed when a second crystal structure was reported, in which a P2X receptor was bound to ATP and resolved in an open channel conformation. This remarkable structure not only confirms many key experimental data, including the recent mechanisms of ATP binding and ion permeation, but also reveals unanticipated mechanisms. Certainly, this new information will accelerate our understanding of P2X receptor function and pharmacology at the atomic level.
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