Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 7, Pages 2178-2182Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.02.042
Keywords
Carbonic anhydrase; Brucella suis; Sulfonamide; Sugar-sulfanilamide; Enzyme inhibitor
Categories
Ask authors/readers for more resources
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.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available