Druggable site near the upper vestibule determines the high affinity and P2X3 homotrimer selectivity of sivopixant/S‐600918 and its analogue DDTPA

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作者信息关键词期刊信息基础信息归属信息摘要

成果类型：

期刊论文

作者：

Wang, Dong-Ping;Zhang, Meng;Li, Ming;Yang, Xiao-Na;Li, Changzhu;...

通讯作者：

Tian, Y;Yu, Ye;Lei, YT

作者机构：

[Tian, Yun; Tian, Y; Wang, Dong-Ping; Zhang, Meng; Yang, Xiao-Na] Hunan Agr Univ, Coll Biosci & Biotechnol, Changsha 410128, Peoples R China.

[Li, Ming; Yu, Ye; Lei, Yun-Tao; Wang, Dong-Ping; Zhang, Meng; Yang, Xiao-Na] China Pharmaceut Univ, Sch Sci, Nanjing 210009, Peoples R China.

[Li, Ming; Yu, Ye; Lei, Yun-Tao; Wang, Dong-Ping; Zhang, Meng; Yang, Xiao-Na] China Pharmaceut Univ, State Key Lab Nat Med, Nanjing 210009, Peoples R China.

[Li, Changzhu] Hunan Acad Forestry, State Key Lab Utilizat Woody Oil Resource, Changsha, Peoples R China.

[Cao, Peng] Nanjing Univ Chinese Med, Hosp Integrated Tradit Chinese & Western Med, Nanjing, Peoples R China.

通讯机构：

[Tian, Y ] H

[Yu, Y; Lei, YT ] C

Hunan Agr Univ, Coll Biosci & Biotechnol, Changsha 410128, Peoples R China.

China Pharmaceut Univ, Sch Sci, Nanjing 210009, Peoples R China.

China Pharmaceut Univ, State Key Lab Nat Med, Nanjing 210009, Peoples R China.

语种：

英文

关键词：

P2X receptors;hP2X2/3 heterotrimers;ligand recognition;refractory chronic cough;sivopixant/S-600918

期刊：

BRITISH JOURNAL OF PHARMACOLOGY

ISSN：

0007-1188

年：

2024

卷：

181

期：

页码：

1203-1220

DOI：

10.1111/bph.16273

基金类别：

National Natural Science Foundation of China; Natural Science Foundation of Jiangsu Province [BK20202002]; Innovation and Entrepreneurship Talent Program of Jiangsu Province; State Key Laboratory of Utilization of Woody Oil Resource [2019XK2002]; Hunan "Huxiang" High-level Talent Program [2021]; CAMS Innovation Fund for Medical Sciences (CIFMS) [2019-I2M-5-074]; Medical Innovation and Development Project of Lanzhou University [lzuyxcx-2022-156]; [32371289]; [31570832]; [31900808]; [KQ2301004]

机构署名：

本校为第一且通讯机构

院系归属：

生物科学技术学院

摘要：

BACKGROUND AND PURPOSE: The P2X3 receptor, a trimeric ionotropic purinergic receptor, has emerged as a potential therapeutic target for refractory chronic cough (RCC). Nevertheless, gefapixant/AF-219, the only marketed P2X3 receptor antagonist, might lead taste disorders by modulating the human P2X2/3 (hP2X2/3) heterotrimer. Hence, in RCC drug development, compounds exhibiting strong affinity for the hP2X3 homotrimer and a weak affinity for the hP2X2/3 heterotrimer hold promise. An example of such a molecule is sivopixant/S-600918, a clinical Phase II RCC candidate with a reduced incidence of ...

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Druggable site near the upper vestibule determines the high affinity and P2X3 homotrimer selectivity of sivopixant/S‐600918 and its analogue DDTPA

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