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