کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1375236 981934 2008 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design, synthesis, and evaluation of bisubstrate analog inhibitors of cholera toxin
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design, synthesis, and evaluation of bisubstrate analog inhibitors of cholera toxin
چکیده انگلیسی

Bisubstrate analog inhibitors in which a nicotinamide mimic is attached to a series of structurally diversified guanidines (arginine mimics) were synthesized and evaluated for inhibition of cholera toxin. The mechanism-based bisubstrate inhibitors were up to 1400-fold more potent than the natural substrate NAD+ and 400-fold more potent than the artificial substrate diethylamino (benzylidine-amino)guanidine (DEABAG) in an assay toward an intrinsically active mutant of wild-type cholera toxin.

Bisubstrate analog inhibitors in which a nicotinamide mimetic is attached to a series of structurally diversified guanidines (arginine mimic) were synthesized and evaluated for inhibition of cholera toxin. Our results demonstrated that the mechanism-based bisubstrate inhibitors were up to 1400-fold more potent than natural substrate NAD+ and 400-fold more potent than the artificial substrate diethylamino (benzylidine-amino)guanidine (DEABAG) in an assay toward an intrinsically active mutant of wild-type cholera toxin.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 13, 1 July 2008, Pages 3724–3727
نویسندگان
,