Rational design and characterization of a Rac GTPase-specific small molecule inhibitor.

By Yuan Gao, J. Dickerson, F. Guo, Jie Zheng, Yi Zheng. Proceedings of the National Academy of Sciences of the United States of America, 2004

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Mechanical tugging force regulates the size of cell–cell junctions (2010, background): “Rac activity can be antagonized using NSC23766, which prevents the interaction of Rac1 and its upstream activators Tiam1 and Trio (36).”
GEFs and GAPs: critical elements in the control of small G proteins. (2007, background): “vivo (Gao et al., 2004).”
GTP‐binding proteins of the Rho/Rac family: regulation, effectors and functions in vivo (2007, background): “The understanding of all these regulatory steps has allowed the development, for the first time, of drugs that can control the signaling output of Rho family GTPases in specific pathological states by interfering with their GDP/GTP exchange,(41) post-translational modification,(8) and sub-cellular l”
Ras superfamily GEFs and GAPs: validated and tractable targets for cancer therapy? (2010, background): “Through computational screening of the surface of RAC1 that is known to interact with GEFs, the small molecule NSC23766 was discovered, which inhibited activation of RAC1 by the Rac-specific GEFs TRIO and TIAM1, but not GEF activation of RHOA or CDC42 in vitro and in cell”