期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 7, 页码 2178-2182出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.02.042
关键词
Carbonic anhydrase; Brucella suis; Sulfonamide; Sugar-sulfanilamide; Enzyme inhibitor
A beta-carbonic anhydrase (CA, EC 4,2,1,1) from the bacterial pathogen Brucella suis, bsCA 1, has been cloned, purified characterized kinetically and for inhibition with a series of water soluble glycosylated sulfanilamides. bsCA 1 has appreciable activity as catalyst for the hydration of CO2 to bicarbonate, with a k(cat) of 6.4 x 10(5) s(-1) and k(cat)/K-m of 3.9 x 10(7) M-1 s(-1). All types of inhibitory activities have been detected, with K(I)s in the range of 8.9-110 nM. The best bsCA 1 inhibitor were the galactose and ribose sulfanilamides, with inhibition constants of 8.9-9.2 nM. Small structural changes in the sugar moiety led to dramatic differences of enzyme inhibitory activity for this series of compounds. One of the tested glycosylsulfonamides and acetazolamide significantly inhibited the growth of the bacteria in cell cultures. (C) 2010 Elsevier Ltd. All rights reserved.
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