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

被引：87

作者：

Young, K

Lin, S

Sun, L

Lee, E

Modi, M

Hellings, S

Husbands, M

Ozenberger, B

Franco, R ^{[1
]}

机构：

[1] Wyeth Ayerst Res, CNS Disorders, Princeton, NJ 08543 USA

[2] Cyanamid Agr Res Ctr, Princeton, NJ 08543 USA

[3] Wyeth Ayerst Res, CNS MCB, Princeton, NJ 08543 USA

来源：

NATURE BIOTECHNOLOGY | 1998年 / 16卷 / 10期

关键词：

drug screen; protein-protein interaction; neurotransmitter;

D O I：

10.1038/nbt1098-946

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

The interaction of the N-type calcium channel beta 3 subunit with the alpha 1B subunit alters the activation/inactivation kinetics and the maximal conductance of the channel. The defined protein-protein interaction of the human alpha 1B and beta 3 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 alpha 1B-beta 3 subunit interactions and Inhibit N-type calcium channel activity. These small molecules may be a new class of calcium channel antagonists with therapeutic potential.

引用

页码：946 / 950

页数：5