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

Young, K; Lin, S; Sun, L; Lee, E; Modi, M; Hellings, S; Husbands, M; Ozenberger, B et al. · Nat Biotechnol · 1998

basic_science · Level V

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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.

Medical subject headings