Structure-functional diversity of human L-type Ca2+ channel: Perspectives for new pharmacological targets

Darrell R. Abernethy, Nikolai M. Soldatov

Research output: Contribution to journalReview articlepeer-review

Abstract

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.

Original languageEnglish (US)
Pages (from-to)724-728
Number of pages5
JournalJournal of Pharmacology and Experimental Therapeutics
Volume300
Issue number3
DOIs
StatePublished - 2002

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology

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