Molecular mechanism underlying the subtype-selectivity of competitive inhibitor NF110 and its distinct potencies in human and rat P2X3 receptors

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成果类型：

期刊论文

作者：

Li, Bin;Wang, Jin;Cheng, Xiaoyang;Liu, Yan;Yang, Yang;...

通讯作者：

Tian, Yun;Yu, Ye

作者机构：

[Tian, Yun; Zhu, Michael X.; Lu, Xiangyang; Yang, Yang; Li, Bin; Yang, Xiaona] Hunan Agr Univ, Coll Biosci & Biotechnol, Changsha 410128, Hunan, Peoples R China.

[Zhu, Michael X.] Guangxi Normal Univ, Sch Chem & Pharmaceut Sci, State Key Lab Chem & Mol Engn Med Resources, Guilin 541004, Peoples R China.

[Cheng, Xiaoyang; Liu, Yan; Li, Bin; Wang, Jin; Yu, Ye] Shanghai Jiao Tong Univ, Inst Med Sci, Dept Pharmacol & Chem Biol, Sch Med, Shanghai 200025, Peoples R China.

[Guo, Changrun; Yu, Ye; Yang, Xiaona] China Pharmaceut Univ, Sch Basic Med & Clin Pharm, Nanjing 210009, Jiangsu, Peoples R China.

[Niu, Youya] Hunan Univ Med, Dept Cell Biol & Genet, Huaihua 418000, Peoples R China.

通讯机构：

[Tian, Yun] H

[Yu, Ye] S

[Yu, Ye] C

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

Shanghai Jiao Tong Univ, Inst Med Sci, Dept Pharmacol & Chem Biol, Sch Med, Shanghai 200025, Peoples R China.

语种：

英文

关键词：

P2X receptors;Competitive inhibitors;NF110;Species-specificity;Subtype-selectivity

期刊：

科学通报(英文版)

ISSN：

2095-9273

年：

2018

卷：

期：

页码：

1616-1625

DOI：

10.1016/j.scib.2018.11.016

基金类别：

National Natural Science Foundation of ChinaNational Natural Science Foundation of China [31570832]; National Program on Key Basic Research Project of ChinaNational Basic Research Program of China [2014CB9103000/02]; Science and Technology Department of Hunan Province [2018RS3086]; National Postdoctoral Program for Innovative Talents [BX201700306]; China Postdoctoral Science FoundationChina Postdoctoral Science Foundation [2018M632127]; Hunan Provincial Natural Science FoundationNatural Science Foundation of Hunan Province [2017JJ2198, 2018JJ1012]; Guangxi Funds for Distinguished Experts

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：

P2X receptors are a family of extracellular ATP-gated trimeric cation channels that is widely distributed in human tissues. Quite some drug candidates targeting P2X receptors have entered into preclinical or main phases of clinical trials, but many of them failed due to low subtype-selectivity or species differences in pharmacological activities between human and experimental animals. Here, we identified the distinct inhibitory efficacies of NF110, a competitive inhibitor, between the rat (rP2X3) and human (hP2X3) P2X3 receptors. We demonstrate...

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Molecular mechanism underlying the subtype-selectivity of competitive inhibitor NF110 and its distinct potencies in human and rat P2X3 receptors

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