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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Review Article

Advances in L-Type Calcium Channel Structures, Functions and Molecular Modeling

Author(s): Lei Xu*, Lilei Sun, Liangxu Xie, Shanzhi Mou, Dawei Zhang, Jingyu Zhu and Peng Xu*

Volume 28, Issue 3, 2021

Published on: 14 July, 2020

Page: [514 - 524] Pages: 11

DOI: 10.2174/0929867327666200714154059

Price: $65


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.

Keywords: L-type calcium channels, voltage-gated calcium channels, isoform-selective VGCC modulators, drugbindingsites, computer-aided drug design, molecular modeling.

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