Literature DB >> 33068968

Inhibition of the newly discovered β‑carbonic anhydrase from the protozoan pathogen Trichomonas vaginalis with inorganic anions and small molecules.

Linda J Urbański1, Andrea Angeli2, Vesa P Hytönen3, Anna Di Fiore4, Seppo Parkkila3, Giuseppina De Simone5, Claudiu T Supuran6.   

Abstract

The protozoan pathogen Trichomonas vaginalis encodes two carbonic anhydrases (CAs, EC 4.2.1.1) belonging to the β-class. One of these enzymes, T. vaginalis carbonic anhydrase 1 (TvaCA1), was recently cloned and characterized by our group, and its X-ray crystal structure reported. No inhibitors of this enzyme were reported up until now. Here we investigated the inhibition of TvaCA1 with inorganic anions and small molecules and observed that thiocyanate, cyanide, selenite, selenocyanate and divanadate are sub-millimolar inhibitors, whereas sulfamide, sulfate, phenylboronic acid and phenylarsonic acid are micromolar inhibitors. Finding effective TvaCA1 inhibitors may be useful for developing new antiprotozoan drugs.
Copyright © 2020 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Anion; Beta-class enzyme; Carbonic anhydrase; Inhibitor; Trichomonas vaginalis; Trichomoniasis

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Year:  2020        PMID: 33068968     DOI: 10.1016/j.jinorgbio.2020.111274

Source DB:  PubMed          Journal:  J Inorg Biochem        ISSN: 0162-0134            Impact factor:   4.155


  3 in total

1.  Gold(I) Phosphine Derivatives with Improved Selectivity as Topically Active Drug Leads to Overcome 5-Nitroheterocyclic Drug Resistance in Trichomonas vaginalis.

Authors:  Yukiko Miyamoto; Shubhangi Aggarwal; Jeff Joseph A Celaje; Sozaburo Ihara; Jonathan Ang; Dmitry B Eremin; Kirkwood M Land; Lisa A Wrischnik; Liangfang Zhang; Valery V Fokin; Lars Eckmann
Journal:  J Med Chem       Date:  2021-05-11       Impact factor: 8.039

2.  Activation of the β-carbonic anhydrase from the protozoan pathogen Trichomonas vaginalis with amines and amino acids.

Authors:  Andrea Angeli; Linda J Urbański; Vesa P Hytönen; Seppo Parkkila; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051

3.  Inhibition of the β-carbonic anhydrase from the protozoan pathogen Trichomonas vaginalis with sulphonamides.

Authors:  Linda J Urbański; Andrea Angeli; Vesa P Hytönen; Anna Di Fiore; Giuseppina De Simone; Seppo Parkkila; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051

  3 in total

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