Development of a novel high-throughput screen and identification of small-molecule inhibitors of the Gα-RGS17 protein-protein interaction using AlphaScreen.

ABSTRACT: In this study, the authors used AlphaScreen technology to develop a high-throughput screening method for interrogating small-molecule libraries for inhibitors of the Gα(o)-RGS17 interaction. RGS17 is implicated in the growth, proliferation, metastasis, and the migration of prostate and lung cancers. RGS17 is upregulated in lung and prostate tumors up to a 13-fold increase over patient-matched normal tissues. Studies show RGS17 knockdown inhibits colony formation and decreases tumorigenesis in nude mice. The screen in this study uses a measurement of the Gα(o)-RGS17 protein-protein interaction, with an excellent Z score exceeding 0.73, a signal-to-noise ratio >70, and a screening time of 1100 compounds per hour. The authors screened the NCI Diversity Set II and determined 35 initial hits, o

SUBMITTER: Mackie DI 

PROVIDER: S-EPMC5525514 | biostudies-literature | 2011 Sep

REPOSITORIES: biostudies-literature