Inhibition of the newly discovered β‑carbonic anhydrase from the protozoan pathogen Trichomonas vaginalis with inorganic anions and small molecules
| Autor: | Seppo Parkkila, Anna Di Fiore, Claudiu T. Supuran, Vesa P. Hytönen, Linda J Urbański, Giuseppina De Simone, Andrea Angeli |
|---|---|
| Přispěvatelé: | Tampere University, BioMediTech, Department of Clinical Chemistry |
| Rok vydání: | 2020 |
| Předmět: |
Anions
Protein Conformation Antiprotozoal Agents 010402 general chemistry medicine.disease_cause 01 natural sciences Biochemistry Small Molecule Libraries Inorganic Chemistry chemistry.chemical_compound Carbonic anhydrase Trichomonas vaginalis medicine Humans Phenylboronic acid Carbonic Anhydrase Inhibitors Sulfamide Carbonic Anhydrases chemistry.chemical_classification biology Thiocyanate 010405 organic chemistry Phenylarsonic acid Small molecule 0104 chemical sciences Enzyme chemistry Inorganic Chemicals biology.protein 1182 Biochemistry cell and molecular biology Female 3111 Biomedicine Trichomonas Vaginitis |
| Zdroj: | Journal of Inorganic Biochemistry. 213:111274 |
| ISSN: | 0162-0134 |
| Popis: | 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. acceptedVersion |
| Databáze: | OpenAIRE |
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