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
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Structure–activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding
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
نویسندگان
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