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Allosteric interactions required for high-affinity binding of dihydropyridine antagonists to Ca(V)1.1 Channels are modulated by calcium in the pore

Allosteric interactions required for high-affinity binding of dihydropyridine antagonists to Ca(V)1.1 Channels are modulated by calcium in the pore

Molecular Pharmacology 70(2): 667-675

ISSN/ISBN: 0026-895X

PMID: 16675661

DOI: 10.1124/mol.105.020644

Dihydropyridines (DHPs) are an important class of drugs, used extensively in the treatment of angina pectoris, hypertension, and arrhythmia. The molecular mechanism by which DHPs modulate Ca2+ channel function is not known in detail. We have found that DHP binding is allosterically coupled to Ca2+ binding to the selectivity filter of the skeletal muscle Ca2+ channel Ca(V)1.1, which initiates excitation-contraction coupling and conducts L-type Ca2+ currents.

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