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.