Structural basis for inhibition of a voltage-gated Ca²⁺ channel by Ca²⁺ antagonist drugs.

ABSTRACT: Ca²⁺ antagonist drugs are widely used in therapy of cardiovascular disorders. Three chemical classes of drugs bind to three separate, but allosterically interacting, receptor sites on Ca_V1.2 channels, the most prominent voltage-gated Ca²⁺ (Ca_V) channel type in myocytes in cardiac and vascular smooth muscle. The 1,4-dihydropyridines are used primarily for treatment of hypertension and angina pectoris and are thought to act as allosteric modulators of voltage-dependent Ca²⁺ channel activation, whereas phenylalkylamines and benzothiazepines are used primarily for treatment of cardiac arrhythmias and are thought to physically block the pore. The structural basis for the different binding, action, and therapeutic uses of these drugs remains

SUBMITTER: Tang L 

PROVIDER: S-EPMC5161592 | biostudies-literature | 2016 Sep

REPOSITORIES: biostudies-literature