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Description: ML098 (also known as CID-7345532) is a potent activator of the GTP-binding protein Rab7 with an EC50 of 77.6 nM. It functions by increasing the affinity of the GTPases for guanine nucleotides, leading to the hypothesis that these activators interact with GTPases bind to an allosteric binding site localized between switch regions I and II. Based on these findings, the project further proposes that in biochemical systems, these novel small activators should prove useful towards: (1) elucidating the mechanism by which GEF regulates GTPase activity; (2) defining protein-protein interactions between GEFs and GTPases; (3) defining the sites of GTPase regulation in crystal structures and (4) platforms for the development of probes that can be used to activate GTPase function.
References: https://www.ncbi.nlm.nih.gov/books/NBK47359/
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