Structural insights into the competitive inhibition of the ATP-gated P2X receptor channel

Structural insights into the competitive inhibition of the ATP-gated P2X receptor channel

P2X receptors are nonselective cation channels that are gated by extracellular ATP. Here the authors present the crystal structure of chicken P2X7 with its bound competitive antagonist TNP-ATP and give mechanistic insights into TNP-ATP dependent inhibition through further computational analysis and...

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Main Authors: Go Kasuya, Toshiaki Yamaura, Xiao-Bo Ma, Ryoki Nakamura, Mizuki Takemoto, Hiromitsu Nagumo, Eiichi Tanaka, Naoshi Dohmae, Takanori Nakane, Ye Yu, Ryuichiro Ishitani, Osamu Matsuzaki, Motoyuki Hattori, Osamu Nureki
Format: article
Language:EN
Published: Nature Portfolio 2017
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Science
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Online Access:https://doaj.org/article/cb0f6ce882154f37b17a413f1ef7ef0d
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Summary:P2X receptors are nonselective cation channels that are gated by extracellular ATP. Here the authors present the crystal structure of chicken P2X7 with its bound competitive antagonist TNP-ATP and give mechanistic insights into TNP-ATP dependent inhibition through further computational analysis and electrophysiology measurements.

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