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:	English
Published:	Nature Publishing Group 2017-10-01
Series:	Nature Communications
Online Access:	https://doi.org/10.1038/s41467-017-00887-9

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spelling	doaj-cb0f6ce882154f37b17a413f1ef7ef0d2021-05-11T07:04:20ZengNature Publishing GroupNature Communications2041-17232017-10-018111010.1038/s41467-017-00887-9Structural insights into the competitive inhibition of the ATP-gated P2X receptor channelGo Kasuya0Toshiaki Yamaura1Xiao-Bo Ma2Ryoki Nakamura3Mizuki Takemoto4Hiromitsu Nagumo5Eiichi Tanaka6Naoshi Dohmae7Takanori Nakane8Ye Yu9Ryuichiro Ishitani10Osamu Matsuzaki11Motoyuki Hattori12Osamu Nureki13Department of Biological Sciences, Graduate School of Science, The University of TokyoLaboratory for Drug Discovery, Pharmaceuticals Research Center, Asahi Kasei Pharma CorporationDepartment of Pharmacology and Chemical Biology, Institute of Medical Sciences, School of Medicine, Shanghai Jiao Tong UniversityDepartment of Biological Sciences, Graduate School of Science, The University of TokyoDepartment of Biological Sciences, Graduate School of Science, The University of TokyoLaboratory for Drug Discovery, Pharmaceuticals Research Center, Asahi Kasei Pharma CorporationLaboratory for Drug Discovery, Pharmaceuticals Research Center, Asahi Kasei Pharma CorporationGlobal Research Cluster, RIKENDepartment of Biological Sciences, Graduate School of Science, The University of TokyoDepartment of Pharmacology and Chemical Biology, Institute of Medical Sciences, School of Medicine, Shanghai Jiao Tong UniversityDepartment of Biological Sciences, Graduate School of Science, The University of TokyoPharmaceuticals Research Center, Asahi Kasei Pharma CorporationState Key Laboratory of Genetic Engineering, Collaborative Innovation Center of Genetics and Development, Department of Physiology and Biophysics, School of Life Sciences, Fudan UniversityDepartment of Biological Sciences, Graduate School of Science, The University of TokyoP2X 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.https://doi.org/10.1038/s41467-017-00887-9
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	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
spellingShingle	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 Structural insights into the competitive inhibition of the ATP-gated P2X receptor channel Nature Communications
author_facet	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
author_sort	Go Kasuya
title	Structural insights into the competitive inhibition of the ATP-gated P2X receptor channel
title_short	Structural insights into the competitive inhibition of the ATP-gated P2X receptor channel
title_full	Structural insights into the competitive inhibition of the ATP-gated P2X receptor channel
title_fullStr	Structural insights into the competitive inhibition of the ATP-gated P2X receptor channel
title_full_unstemmed	Structural insights into the competitive inhibition of the ATP-gated P2X receptor channel
title_sort	structural insights into the competitive inhibition of the atp-gated p2x receptor channel
publisher	Nature Publishing Group
series	Nature Communications
issn	2041-1723
publishDate	2017-10-01
description	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.
url	https://doi.org/10.1038/s41467-017-00887-9
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Structural insights into the competitive inhibition of the ATP-gated P2X receptor channel

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