کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1371853 | 981857 | 2009 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Structure–activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
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.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 19, 1 October 2009, Pages 5594–5598
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 19, 1 October 2009, Pages 5594–5598
نویسندگان
Eric Beausoleil, 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,