TY - JOUR T1 - Structure-Functional Diversity of Human L-Type Ca<sup>2+</sup>Channel: Perspectives for New Pharmacological Targets JF - Journal of Pharmacology and Experimental Therapeutics JO - J Pharmacol Exp Ther SP - 724 LP - 728 DO - 10.1124/jpet.300.3.724 VL - 300 IS - 3 AU - Darrell R. Abernethy AU - Nikolai M. Soldatov Y1 - 2002/03/01 UR - http://jpet.aspetjournals.org/content/300/3/724.abstract N2 - The L-type Ca2+ channels mediate depolarization-induced influx of Ca2+ into a wide variety of cells and thus play a central role in triggering cardiac and smooth muscle contraction. Because of this role, clinically important classes of 1,4-dihydropyridine, phenylalkylamine, and benzothiazepine Ca2+ channel blockers were developed as powerful medicines to treat hypertension and angina pectoris. Molecular cloning studies revealed that the channel is subject to extensive structure-functional variability due to alternative splicing. In this review, we will focus on a potentially important role of genetically driven variability of Ca2+ channels in expression regulation and mutations, Ca2+-induced inactivation, and modulation of sensitivity to Ca2+ channel blockers with the perspective for new pharmacological targets. U.S. Government ER -