Discovery of MINC1, a GTPase-Activating Protein Small Molecule Inhibitor, Targeting MgcRacGAP

van Adrichem A, et al., 18(1):3-17, Comb Chem High Throughput Screen, 2015

The identification of a Male germ cell Rac GTPase-activating protein (MgcRacGAP) inhibitor with the hope of dissecting its biological role is reported. The interaction between MgcRacGAP and Rac1 (Q61L) was analyzed using a Pall ForteBio Octet RED384 system equipped with Anti-GST biosensor probes. MgcRacGAP, together with Rac1 and two other protein candidates, regulates mitosis. The MgcRacGAP labeled with a GST is loaded onto the Anti-GST biosensors and analyzed against Rac1Q61L. The discovery of this inhibitor (MINC1) and its ability to interfere with biological functions of the protein in cells suggest the possibility of developing inhibitors for other small GTPase GAPs.

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