NDLI: Characterization of a Cdc42 Protein Inhibitor and Its Use as a Molecular $Probe^{*}$

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Characterization of a Cdc42 Protein Inhibitor and Its Use as a Molecular $Probe^{*}$

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Swanson, Scarlett Chigaev, Alexandre Wandinger-ness, Angela Schroeder, Chad E. Hjelle, Brian Aubé, Jeffrey Kenney, S. Ray Nöth, Julica Ursu, Oleg Sklar, Larry A. Hudson, Laurie G. Oprea, Tudor Phillips, Genevieve K. Hong, Lin Romero, Elsa Strouse, J. Jacob Carter, Mark Buranda, Tione Simpson, Denise Golden, Jennifer E. Waller, Anna
Description	Author Affiliation: Hong L ( Department of Pathology, University of New Mexico, Albuquerque, New Mexico 87131, USA.)
Abstract	Cdc42 plays important roles in cytoskeleton organization, cell cycle progression, signal transduction, and vesicle trafficking. Overactive Cdc42 has been implicated in the pathology of cancers, immune diseases, and neuronal disorders. Therefore, Cdc42 inhibitors would be useful in probing molecular pathways and could have therapeutic potential. Previous inhibitors have lacked selectivity and trended toward toxicity. We report here the characterization of a Cdc42-selective guanine nucleotide binding lead inhibitor that was identified by high throughput screening. A second active analog was identified via structure-activity relationship studies. The compounds demonstrated excellent selectivity with no inhibition toward Rho and Rac in the same GTPase family. Biochemical characterization showed that the compounds act as noncompetitive allosteric inhibitors. When tested in cellular assays, the lead compound inhibited Cdc42-related filopodia formation and cell migration. The lead compound was also used to clarify the involvement of Cdc42 in the Sin Nombre virus internalization and the signaling pathway of integrin VLA-4. Together, these data present the characterization of a novel Cdc42-selective allosteric inhibitor and a related analog, the use of which will facilitate drug development targeting Cdc42-related diseases and molecular pathway studies that involve GTPases.
ISSN	00219258
e-ISSN	1083351X
Journal	Journal of Biological Chemistry
Issue Number	12
Volume Number	288
Language	English
Publisher	American Society for Biochemistry and Molecular Biology (United States)
Publisher Date	2013-03-22
Publisher Place	United States
Access Restriction	Open
Subject Keyword	Enzyme Inhibitors Pharmacology Molecular Probes Pyrazoles Sulfonamides Cdc42 GTP-Binding Protein Antagonists & Inhibitors 3T3 Cells Allosteric Regulation Animals Antiviral Agents Cell Line, Tumor Cell Movement Drug Effects Cell Survival Enzyme Activation Integrin Alpha4beta1 Physiology Mice Oligopeptides Metabolism Phenylurea Compounds Protein Binding Pseudopodia Sin Nombre Virus Structure-Activity Relationship Virus Internalization Chemistry Rac1 GTP-Binding Protein RhoA GTP-Binding Protein Research Support, N.I.H., Extramural Research Support, Non-U.S. Gov't Research Support, U.S. Gov't, Non-P.H.S. Biochemistry Molecular Biology
Content Type	Text
Resource Type	Article
Subject	Cell Biology Biochemistry Molecular Biology

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