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药物研发中的瞬时受体电位(TRP)通道:旧概念与新思考

Transient Receptor Potential (TRP) Channels in Drug Discovery: Old Concepts & New Thoughts.

作者信息

Huang Susan, Szallasi Arpad

机构信息

AbbVie Inc, 1 North Waukegan Road, North Chicago, IL 60064, USA.

Baptist Medical Center, 800 Prudential Drive, Jacksonville, FL 32207, USA.

出版信息

Pharmaceuticals (Basel). 2017 Jul 6;10(3):64. doi: 10.3390/ph10030064.

Abstract

2017 marks the 20th anniversary of the molecular cloning by David Julius and colleagues (1997) of the long sought-after capsaicin receptor, now known as TRPV1 (Transient Receptor Potential Vanilloid 1) [1]. This seminal discovery has opened up a "hot" new field of basic research and launched drug discovery efforts into the large family (by the latest count 28 mammalian members, 27 in humans) of TRP ion channels [2]. Indeed, it took less than a decade for the first potent, small molecule TRPV1 antagonists to enter phase 1 clinical trials [3]. Yet, despite the large amount of resources that has been invested in TRPV1 research, there are currently no TRPV1-targeted drugs in phase 3 clinical trials. In this special issue of Pharmaceuticals, we aim to capture the progress in the TRP channel field over the past twenty years, with 15 articles covering a variety of TRP channels and potential relevant disease states and applications.

摘要

2017年是大卫·朱利叶斯及其同事在1997年成功克隆长期以来备受追寻的辣椒素受体的20周年纪念,该受体现在被称为TRPV1(瞬时受体电位香草酸亚型1)[1]。这一开创性的发现开启了一个全新的基础研究“热门”领域,并推动了针对TRP离子通道大家族(最新统计有28个哺乳动物成员,人类有27个)的药物研发工作[2]。事实上,不到十年时间,首批强效小分子TRPV1拮抗剂就进入了1期临床试验[3]。然而,尽管在TRPV1研究上投入了大量资源,但目前尚无TRPV1靶向药物进入3期临床试验。在本期《药物》特刊中,我们旨在总结过去二十年来TRP通道领域的进展,共有15篇文章涵盖了各种TRP通道以及潜在的相关疾病状态和应用。

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本文引用的文献

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TRPV3 in Drug Development.药物研发中的瞬时受体电位香草酸亚型3(TRPV3)
Pharmaceuticals (Basel). 2016 Sep 9;9(3):55. doi: 10.3390/ph9030055.
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TRPV1: A Target for Rational Drug Design.TRPV1:理性药物设计的靶点。
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