Lei Xu*, Lilei Sun, Liangxu Xie, Shanzhi Mou, Dawei Zhang, Jingyu Zhu and Peng Xu* Pages 514 - 524 ( 11 )
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.
L-type calcium channels, voltage-gated calcium channels, isoform-selective VGCC modulators, drugbindingsites, computer-aided drug design, molecular modeling.
Institute of Bioinformatics and Medical Engineering, School of Electrical and Information Engineering, Jiangsu University of Technology, Changzhou 213001, Department of Radiology, Weifang Second People's Hospital, Weifang 261041, Institute of Bioinformatics and Medical Engineering, School of Electrical and Information Engineering, Jiangsu University of Technology, Changzhou 213001, School of Mathematics and Physics, Jiangsu University of Technology, Changzhou 213001, Institute of Bioinformatics and Medical Engineering, School of Electrical and Information Engineering, Jiangsu University of Technology, Changzhou 213001, School of Medicine and Pharmaceutics, Jiangnan University, Wuxi 214122, Department of Orthopedics, Second Military Medical University Affiliated Changzheng Hospital, Shanghai 200003