beta-Subunits: fine tuning of Ca(2+) channel block.
Ca(2+) channel blockers such as 1,4-dihydropyridines, phenylalkylamines, diltiazem and mibefradil exert their anti-arrhythmic and anti-hypertensive action by restricting Ca(2+) entry into myocardial cells and smooth muscle cells. Binding sites for these drugs are present on the pore-forming alpha(1)-subunits of voltage-dependent Ca(2+) (Ca(v)) channels. However, striking new data show that auxillary beta-subunits also influence drug sensitivity significantly. These findings are summarized and the underlying molecular mechanisms and their pharmacological relevance are discussed.
Hering
Steffen
S
Institut für Biochemische Pharmakologie, Peter Mayr Strasse 1, A-6020, Innsbruck, Austria. Steffen.Hering@uibk.ac.at
D002121:Calcium Channel Blockers / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D008968:Molecular Conformation; D013329:Structure-Activity Relationship
D002121:Calcium Channel Blockers