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.
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Authors | Darrell R Abernethy, Nikolai M Soldatov |
Journal | The Journal of pharmacology and experimental therapeutics
(J Pharmacol Exp Ther)
Vol. 300
Issue 3
Pg. 724-8
(Mar 2002)
ISSN: 0022-3565 [Print] United States |
PMID | 11861774
(Publication Type: Journal Article, Review)
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Chemical References |
- Calcium Channel Blockers
- Calcium Channels, L-Type
- Dihydropyridines
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Topics |
- Amino Acid Sequence
- Animals
- Calcium Channel Blockers
(pharmacology)
- Calcium Channels, L-Type
(chemistry, drug effects, genetics, metabolism)
- Dihydropyridines
(chemistry, pharmacology)
- Genome
- Humans
- Molecular Sequence Data
- Promoter Regions, Genetic
- Structure-Activity Relationship
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