Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.

Abstract

The synthesis of a series of berberine, phenantridine and isoquinoline derivatives was realized to explore their Rho GTPase nucleotide inhibitory activity. The compounds were evaluated in a nucleotide binding competition assay against Rac1, Rac1b, Cdc42 and in a cellular Rac GTPase activation assay. The insertion of 19 AA in the splice variant Rac1b is… (More)
DOI: 10.1016/j.bmcl.2009.08.037

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@article{Beausoleil2009StructureactivityRO, title={Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.}, author={Eric Beausoleil and C{\'e}dric Chauvignac and Thierry Taverne and Sandrine Lacombe and Laure Pognante and Bertrand Leblond and Diego Pallares and Catherine De Oliveira and Florence Bachelot and Rachel Carton and H{\'e}l{\`e}ne Peillon and S{\'e}verine Coutadeur and Virginie Picard and Nathalie Lambeng and Laurent D{\'e}sir{\'e} and Fabien Schweighoffer}, journal={Bioorganic & medicinal chemistry letters}, year={2009}, volume={19 19}, pages={5594-8} }