l型钙通道结构、功能及分子模拟研究进展。

IF 3.5 4区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Current medicinal chemistry Pub Date : 2021-01-01 DOI:10.2174/0929867327666200714154059
Lei Xu, Lilei Sun, Liangxu Xie, Shanzhi Mou, Dawei Zhang, Jingyu Zhu, Peng Xu
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引用次数: 5

摘要

l型钙通道(ltcc),也称为Cav1,属于电压门控钙通道(VGCCs/Cavs),在广泛的生理过程中发挥关键作用,包括神经传递、细胞周期、肌肉收缩、心脏动作电位和基因表达。钙通道的异常调节与神经、心血管、肌肉和精神疾病有关。因此,LTCC已被视为重要的药物靶点,许多LTCC药物已进入临床应用。本文就近年来ltcc的结构和生物学功能的研究进展作一综述。此外,还讨论了ltcc的代表性调节剂和配体结合位点。最后,综述了分子模型和计算机辅助药物设计(CADD)方法对ltcc结构-功能关系的理解。
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Advances in L-Type Calcium Channel Structures, Functions and Molecular Modeling.

L-type Calcium Channels (LTCCs), also termed as Cav1, belong to voltage-gated calcium channels (VGCCs/Cavs), which play a critical role in a wide spectrum of physiological processes, including neurotransmission, cell cycle, muscular contraction, cardiac action potential and gene expression. Aberrant regulation of calcium channels is involved in neurological, cardiovascular, muscular and psychiatric disorders. Accordingly, LTCCs have been regarded as important drug targets, and a number of LTCC drugs are in clinical use. In this review, the recent development of structures and biological functions of LTCCs are introduced. Moreover, the representative modulators and ligand binding sites of LTCCs are discussed. Finally, molecular modeling and Computer-aided Drug Design (CADD) methods for understanding structure-function relations of LTCCs are summarized.

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来源期刊
Current medicinal chemistry
Current medicinal chemistry 医学-生化与分子生物学
CiteScore
8.60
自引率
2.40%
发文量
468
审稿时长
3 months
期刊介绍: Aims & Scope Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews and guest edited thematic issues written by leaders in the field covering a range of the current topics in medicinal chemistry. The journal also publishes reviews on recent patents. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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