کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10585203 981364 2012 9 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis of deguelin-biotin conjugates and investigation into deguelin's interactions
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis of deguelin-biotin conjugates and investigation into deguelin's interactions
چکیده انگلیسی
Deguelin, a rotenoid, has emerged as an attractive pharmacophore for chemoprevention showing in vivo activity in several xenografts. Recently, several lines of evidence have suggested its mode of action may involve inhibition of HSP90, however binding in a different mode than known pharmacophores. To further probe the target of deguelin and related rotenoids, several biotin conjugates were prepared. None of the conjugates showed significant affinity for HSP90, however two conjugates showed a strong cellular co-localization with mitochondria, consistent with binding to mitochondrial complex 1. Contrarily to rotenone, deguelin and tephrosin were not found to inhibit tubulin polymerization demonstrating a dramatic pharmacological difference between these closely related rotenoids.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 2, 15 January 2012, Pages 672-680
نویسندگان
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