治疗疼痛的n型钙通道调节剂的发现与开发进展。

Q1 Pharmacology, Toxicology and Pharmaceutics Progress in medicinal chemistry Pub Date : 2014-01-01 DOI:10.1016/B978-0-444-63380-4.00004-4

Margaret S Lee

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引用次数: 25

摘要

电压门控钙通道(VGCCs)在心脏和神经功能等基本生理过程中的重要性引起了人们对这些蛋白作为药物干预靶点的强烈兴趣。n型钙通道是vgcc的一个子集，其生理学、药理学和对慢性疼痛的病理意义是不同的。尽管经过数十年的研究，目前只有一种针对n型通道功能的药物进入市场。这篇综述将总结我们目前对n型钙通道的生物学、生理学和药理学的理解以及这些特征对治疗干预的意义。在此基础上，将讨论最近发现和开发n型钙通道功能的肽基和小分子调节剂的工作。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Recent progress in the discovery and development of N-type calcium channel modulators for the treatment of pain.

The importance of voltage-gated calcium channels (VGCCs) in basic physiological processes such as cardiac and neurological function has generated intense interest in these proteins as targets of pharmacological intervention. N-type calcium channels are a subset of VGCCs distinguished by their physiology, pharmacology and significance to the pathology of chronic pain. Despite decades of investigation, only a single drug targeting N-type channel function has entered the marketplace. This review will summarize our current understanding of the biology, physiology and pharmacology of N-type calcium channels and the implication of these features for therapeutic intervention. From this basis of understanding, recent efforts to discover and develop peptide based and small molecule modulators of N-type calcium channel function will be discussed.

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来源期刊

Progress in medicinal chemistry Pharmacology, Toxicology and Pharmaceutics-Pharmacology

CiteScore

15.60

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0.00%

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期刊介绍： This series has a long established reputation for excellent coverage of almost every facet of Medicinal Chemistry and is one of the most respected and instructive sources of information on the subject. The latest volume certifies to the continuing success of a unique series reflecting current progress in a broadly developing field of science.

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