کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1375236 | 981934 | 2008 | 4 صفحه PDF | دانلود رایگان |

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
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 13, 1 July 2008, Pages 3724–3727