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Contribution to Book
A Potent and Selective Inhibitor of Cdc42 GTPase
Pharmacy Faculty Publications
  • Zurab Surviladze, University of New Mexico
  • Anna Waller, University of New Mexico
  • J. Jacob Strouse, University of New Mexico
  • Cristian G. Bologa, University of New Mexico
  • Oleg Ursu, University of New Mexico
  • Virginia M. Salas, University of New Mexico
  • Genevieve K. Phillips, University of New Mexico
  • John F. Parkinson, University of New Mexico
  • Elsa Romero, University of New Mexico
  • Angela Wandinger-Ness, University of New Mexico
  • Larry A. Sklar, University of New Mexico
  • Chad E. Schroeder, University of Kansas
  • Denise S. Simpson, Cedarville University
  • Julica Nöth, University of Kansas
  • Jenna Wang, University of Kansas
  • Jennifer E. Golden, University of Kansas
  • Jeffrey Aubé, University of Kansas
Document Type
Web Publication
Publication Date
1-1-2010
Keywords
  • Cdc42,
  • GTPase,
  • Rho family
Abstract

Cdc42, a member of the Rho family of GTPases, has been shown to play a role in cell adhesion, cytoskeletal arrangement, phagocytosis and cell motility and migration, in addition to a host of other diverse biological processes. The function of Rho-family GTPases in disease pathogenesis has been well established and identification of small, cell permeable molecules that selectively and reversibly regulate Rho GTPases is of high scientific and potentially therapeutic interest. There has been limited success in identifying inhibitors that specifically interact with small Rho family GTPases. The identified probe, ML141 (CID-2950007), is demonstrated to be a potent, selective and reversible non-competitive inhibitor of Cdc42 GTPase suitable for in vitro assays, with low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). Given the highly complementary nature of the function of the Rho family GTPases, Cdc42 selective inhibitors such as those reported here should help untangle the roles of the proteins in this family.

PubMed ID
21433396
Comments

In Probe Reports from the NIH Molecular Libraries Program. Bethesda, MD: National Center for Biotechnology Information, 2010.

Citation Information
2010: Surviladze, Z., Waller A., Strouse, J., Bologa, C., & Ursu, O., A Potent and Selective Inhibitor of Cdc42 GTPase, submitted to National Institutes of Health.