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Nat Biotechnol. 1998 Oct;16(10):946-50.

Identification of a calcium channel modulator using a high throughput yeast two-hybrid screen.

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  • 1Wyeth-Ayerst Research, CNS Disorders, Princeton, NJ 08543, USA.

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  • Nat Biotechnol 1998 Nov;16(11):1074.

Abstract

The interaction of the N-type calcium channel beta3 subunit with the alpha1B subunit alters the activation/inactivation kinetics and the maximal conductance of the channel. The defined protein-protein interaction of the human alpha1B and beta3 subunits provides a target for small-molecule modulation of N-type channel activity. We describe a high throughput screen based on a counterselection yeast two-hybrid assay, which was used to identify small molecules that disrupt alpha1B-beta3 subunit interactions and inhibit N-type calcium channel activity. These small molecules may be a new class of calcium channel antagonists with therapeutic potential.

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PMID:
9788351
[PubMed - indexed for MEDLINE]
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