Cyclic Peptides as T-Type Calcium Channel Blockers: Characterization and Molecular Mapping of the Binding Site.

ABSTRACT: T-type calcium (Ca_V3) channels play a crucial role in the generation and propagation of action potentials in excitable cells and are considered potential drug targets for the treatment of neurological and cardiovascular diseases. Given the limited pharmacological repertoire for these channels, there is a great need for novel potent and selective Ca_V3 channel inhibitors. In this study, we used Xenopus oocytes to heterologously express Ca_V3.1 channels and characterized the interaction with a small cyclic peptide, PnCS1. Using molecular modeling, PnCS1 was docked into the cryo-electron microscopy structure of the human Ca_V3.1 channel and molecular dynamics were performed on the resultant complex. The binding site of the peptide was mapped wit

SUBMITTER: Depuydt AS 

PROVIDER: S-EPMC8369677 | biostudies-literature | 2021 Aug

REPOSITORIES: biostudies-literature