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Ref Type Journal Article
PMID (26247207)
Authors Hong L, Guo Y, BasuRay S, Agola JO, Romero E, Simpson DS, Schroeder CE, Simons P, Waller A, Garcia M, Carter M, Ursu O, Gouveia K, Golden JE, Aube J, Wandinger-Ness A, Sklar LA
Title A Pan-GTPase Inhibitor as a Molecular Probe.
Journal Vol Issue Date Pages Journal Short Title
PloS one 10 8 2015 e0134317 PLoS One
URL
Abstract Text Overactive GTPases have often been linked to human diseases. The available inhibitors are limited and have not progressed far in clinical trials. We report here a first-in-class small molecule pan-GTPase inhibitor discovered from a high throughput screening campaign. The compound CID1067700 inhibits multiple GTPases in biochemical, cellular protein and protein interaction, as well as cellular functional assays. In the biochemical and protein interaction assays, representative GTPases from Rho, Ras, and Rab, the three most generic subfamilies of the GTPases, were probed, while in the functional assays, physiological processes regulated by each of the three subfamilies of the GTPases were examined. The chemical functionalities essential for the activity of the compound were identified through structural derivatization. The compound is validated as a useful molecular probe upon which GTPase-targeting inhibitors with drug potentials might be developed.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
CID1067700 CID1067700 0 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
CID1067700 ML282|CID-1067700 RAS Inhibitor (Pan) 10 CID1067700 is a small molecule that inhibits GTP binding to multiple GTPases, including Ras, Rho, and Rab7, blocking downstream signaling, and potentially resulting in decreased cell viability in culture (PMID: 26247207, PMID: 30315251).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References