Discovery of MINC1, a GTPase-activating protein small molecule inhibitor, targeting MgcRacGAP.

ABSTRACT: The Rho family of Ras superfamily small GTPases regulates a broad range of biological processes such as migration, differentiation, cell growth and cell survival. Therefore, the availability of small molecule modulators as tool compounds could greatly enhance research on these proteins and their biological function. To this end, we designed a biochemical, high throughput screening assay with complementary follow-up assays to identify small molecule compounds inhibiting MgcRacGAP, a Rho family GTPase activating protein involved in cytokinesis and transcriptionally upregulated in many cancers. We first performed an in-house screen of 20,480 compounds, and later we tested the assay against 342,046 compounds from the NIH Molecular Libraries Small Molecule Repository. Primary screening hit rate

SUBMITTER: van Adrichem AJ 

PROVIDER: S-EPMC4435052 | biostudies-literature | 2015

REPOSITORIES: biostudies-literature