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Anion inhibition studies of a β-carbonic anhydrase from Clostridium perfringens.

Abstract：

:A β-carbonic anhydrases (CAs, EC 4.2.1.1) was recently cloned, purified and characterized kinetically in the pathogen Clostridium perfringens. We report here the first inhibition study of this enzyme (CpeCA). CpeCA was poorly inhibited by iodide and bromide, and was inhibited with KIs in the range of 1-10mM by a range of anions such as (thio)cyanate, azide, bicarbonate, nitrate, nitrite, hydrogensulfite, hydrogensulfide, stannate, tellurate, pyrophosphate, divanadate, tetraborate, peroxydisulfate, sulfate, iminodisulfonate and fluorosulfonate. Better inhibitory power, with K(I)s of 0.36-1.0 mM, was observed for cyanide, carbonate, selenate, selenocyanide, trithiocarbonate and diethyldithiocarbamate, whereas the best CpeCA inhibitors were sulfamate, sulfamide, phenylboronic acid and phenylarsonic acid, which had KIs in the range of 7-75 μM. This study thus provides the basis for developing better clostridial enzyme inhibitors with potential as antiinfectives with a new mechanism of action.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Vullo D,Sai Kumar RS,Scozzafava A,Capasso C,Ferry JG,Supuran CT

doi

10.1016/j.bmcl.2013.10.037

subject

Has Abstract

pub_date

2013-12-15 00:00:00

pages

6706-10

issue

24

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(13)01243-2

journal_volume

23

pub_type

杂志文章

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