| Literature DB >> 19716293 |
Eric Beausoleil1, Cédric Chauvignac, Thierry Taverne, Sandrine Lacombe, Laure Pognante, Bertrand Leblond, Diego Pallares, Catherine De Oliveira, Florence Bachelot, Rachel Carton, Hélène Peillon, Séverine Coutadeur, Virginie Picard, Nathalie Lambeng, Laurent Désiré, Fabien Schweighoffer.
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 shown to be sufficient to introduce a conformational difference that allows compounds 4, 21, 22, and 26 to exhibit selective inhibition of Rac 1b over Rac1.Entities:
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Year: 2009 PMID： 19716293 DOI： 10.1016/j.bmcl.2009.08.037
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823