| Autor: |
Beausoleil E; Exonhit Therapeutics, 65 Boulevard Massena, F-75013 Paris, France. eric.beausoleil@exonhit.com, Chauvignac C, Taverne T, Lacombe S, Pognante L, Leblond B, Pallares D, Oliveira CD, Bachelot F, Carton R, Peillon H, Coutadeur S, Picard V, Lambeng N, Désiré L, Schweighoffer F |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Oct 01; Vol. 19 (19), pp. 5594-8. Date of Electronic Publication: 2009 Aug 13. |
| DOI: |
10.1016/j.bmcl.2009.08.037 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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