1. Anion inhibition studies of the Zn(II)-bound ι-carbonic anhydrase from the Gram-negative bacterium Burkholderia territorii
- Author
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Claudiu T. Supuran, Viviana De Luca, Andrea Scaloni, Clemente Capasso, Alessio Nocentini, and Andrea Petreni
- Subjects
Anions ,Stereochemistry ,Burkholderia ,RM1-950 ,medicine.disease_cause ,01 natural sciences ,Arsenicals ,Catalysis ,Small Molecule Libraries ,Bacterial Proteins ,Gram negative bacterium ,Carbonic anhydrase ,Drug Discovery ,medicine ,Burkholderia territorii ,Carbonic Anhydrases ,Pharmacology ,Sulfonamides ,biology ,010405 organic chemistry ,Chemistry ,Tin Compounds ,General Medicine ,anion ,Carbon Dioxide ,biology.organism_classification ,Boronic Acids ,Recombinant Proteins ,0104 chemical sciences ,ι-class ,inhibitor ,010404 medicinal & biomolecular chemistry ,Zinc ,?-class ,biology.protein ,Therapeutics. Pharmacology ,Sulfonic Acids ,Bacteria ,Research Article ,Research Paper - Abstract
Burkholderia territorii, a Gram-negative bacterium, encodes for the ι-class carbonic anhydrase (CA, EC 4.2.1.1) BteCAι, which was recently characterised. It acts as a good catalyst for the hydration of CO2 to bicarbonate and protons, with a kcat value of 3.0 × 105 s−1 and kcat/KM value of 3.9 × 107 M−1 s−1. No inhibition data on this new class of enzymes are available to date. We report here an anion and small molecules inhibition study of BteCAι, which we prove to be a zinc(II)- and not manganese(II)-containing enzyme, as reported for diatom ι-CAs. The best inhibitors were sulphamic acid, stannate, phenylarsonic acid, phenylboronic acid and sulfamide (KI values of 6.2–94 µM), whereas diethyldithiocarbamate, tellurate, selenate, bicarbonate and cyanate were submillimolar inhibitors (KI values of 0.71–0.94 mM). The halides (except iodide), thiocyanate, nitrite, nitrate, carbonate, bisulphite, sulphate, hydrogensulfide, peroxydisulfate, selenocyanate, fluorosulfonate and trithiocarbonate showed KI values in the range of 3.1–9.3 mM.
- Published
- 2021
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