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

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Abstract
The interaction of the N-type calcium channel β3 subunit with the α1B subunit alters the activation/inactivation kinetics and the maximal conductance of the channel. The defined protein-protein interaction of the human α1B and β3 subunits provides a target for small-molecule modulation of N-type channel activity. We describe a high throughput screen based on a counterseiection yeast two-hybrid assay, which was used to identify small molecules that disrupt α1B-β3 subunit interactions and inhibit N-type calcium channel activity. These small molecules may be a new class of calcium channel antagonists with therapeutic potential.