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T 型通道药物研发的十字路口。

T-Type Channel Druggability at a Crossroads.

机构信息

Institute of Organic Chemistry and Biochemistry , Czech Academy of Sciences , Prague 166 10 , Czech Republic.

Hotchkiss Brain Institute and Alberta Children's Hospital Research Institute, Cumming School of Medicine , University of Calgary , Calgary T2N4N1 , Canada.

出版信息

ACS Chem Neurosci. 2019 Mar 20;10(3):1124-1126. doi: 10.1021/acschemneuro.9b00031. Epub 2019 Jan 30.

Abstract

Low-voltage activated T-type calcium channels mediate essential functions in the nervous system, and alteration of channel activity is causally linked to a number of neurological conditions. Therefore, T-type channels hold great promise as pharmacological targets for new medicines. In this Viewpoint, we discuss the potential of T-type channels as druggable targets and reevaluate the strategies available for developing therapeutically efficient and specific modulators of this channel.

摘要

低电压激活的 T 型钙通道在神经系统中介导基本功能,通道活性的改变与许多神经疾病有因果关系。因此,T 型通道作为新药的药理学靶点具有很大的潜力。在本观点中,我们讨论了 T 型通道作为可成药靶点的潜力,并重新评估了开发这种通道治疗有效和特异性调节剂的现有策略。

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