Background: By integrating extracellular signals with actin cytoskeletal changes, Cdc42 plays important roles in cell physiology and has been implicated in human diseases.Results: A small molecule was found to selectively inhibit Cdc42 in biochemical and cellular assays.Conclusion: The identified compound is a highly Cdc42-selective inhibitor.Significance: The described first-in-class Cdc42 GTPase-selective inhibitor will have applications in drug discovery and fundamental research.
The revised Fig. 1A correctly shows CID44216842 as a 3-methoxyphenyl analog and not a 4-methoxyphenyl analog as originally published. The correction does not impact the interpretations or conclusions of the article.
A three-component method for synthesizing highly-substituted γ-lactams from readily available maleimides, aldehydes and amines is described. A new reductive amination/intramolecular lactamization sequence provides a straightforward route to the lactam products in a single manipulation. The general utility of this method is demonstrated by the parallel synthesis of a γ-lactam library.
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