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Design, synthesis, and evaluation of bisubstrate analog inhibitors of cholera toxin.

Abstract：

: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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Zhang G

doi

10.1016/j.bmcl.2008.05.049

subject

Has Abstract

pub_date

2008-07-01 00:00:00

pages

3724-7

issue

13

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(08)00548-9

journal_volume

18

pub_type

杂志文章

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