Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 37, Issue 1, Pages 2092-2098Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2022.2101644
Keywords
Carbonic anhydrases; sulphonamide; inhibitor; phenol-sulphuric acid assay; glucose consumption; bacterial growth; microorganism lifecycle
Funding
- Italian Ministry for University and Research (MIUR) [FISR2019_04819 BacCAD]
Ask authors/readers for more resources
Carbonic anhydrases play a crucial role in maintaining metabolic functions in organisms, with inhibitors like acetazolamide able to impair bacterial growth and metabolism.
Carbonic anhydrases, catalysing the reversible CO2 hydration reaction, contribute in all living organisms to the maintenance of stable metabolic functions depending on intracellular concentrations of carbon dioxide, bicarbonate, and protons. Recent studies have examined how CAs affect bacterial lifecycle, considering these enzymes druggable targets due to interference with their activities by using inhibitors or activators. Here, we propose Escherichia coli cells as a model for testing the effect of acetazolamide (AZA), a potent CA inhibitor, on bacterial survival by evaluating E. coli growth through its glucose consumption. AZA, at concentrations higher than 31.2 mu g/mL, was able to impair E. coli growth and glucose uptake. AZA is a good inhibitor of the two recombinant E. coli CAs, the beta-CA CynT2, and the gamma-CA EcoCA gamma, with KIs of 227 and 248 nM, respectively. This study provides a proof-of-concept, low-cost method for identifying effective CA inhibitors capable of impairing bacterial metabolism.
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