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Activation studies with amines and amino acids of the α-carbonic anhydrase from the pathogenic protozoan Trypanosoma cruzi.
Angeli, Andrea; Kuuslahti, Marianne; Parkkila, Seppo; Supuran, Claudiu T.
Afiliação
  • Angeli A; Università degli Studi di Firenze, Dipartimento Neurofarba, Sezione di Scienze Farmaceutiche e Nutraceutiche, Via U. Schiff 6, 50019 Sesto Fiorentino, Florence, Italy.
  • Kuuslahti M; Faculty of Medicine and Life Sciences, University of Tampere, Fimlab Ltd., Tampere University Hospital, 33520 Tampere, Finland.
  • Parkkila S; Faculty of Medicine and Life Sciences, University of Tampere, Fimlab Ltd., Tampere University Hospital, 33520 Tampere, Finland.
  • Supuran CT; Università degli Studi di Firenze, Dipartimento Neurofarba, Sezione di Scienze Farmaceutiche e Nutraceutiche, Via U. Schiff 6, 50019 Sesto Fiorentino, Florence, Italy. Electronic address: claudiu.supuran@unifi.it.
Bioorg Med Chem ; 26(14): 4187-4190, 2018 08 07.
Article em En | MEDLINE | ID: mdl-30007565
ABSTRACT
The activation of a α-class carbonic anhydrase (CAs, EC 4.2.1.1) from Trypanosoma cruzi (TcCA) was investigated with the best known classes of activators, the amino acids and aromatic/heterocyclic amines. The best TcCA activators were l-/d-DOPA and 4-amino-l-phenylalanine, which had activation constants in the range of 0.38-0.83 µM. Low micromolar activators were also l-/d-Trp, l-/d-Tyr, l-Gln, histamine and serotonin (KAs of 1.79-4.92 µM), whereas l-/d-His, l-/d-Phe and l-Asp were less effective activators (KAs of 6.39-18.7 µM). Amines such as dopamine, pyridyl-alkylamines, aminoethyl-piperazine or l-adrenaline, were devoid of activating effects on TcCA. Since the role of autacoids as many of these compounds investigated here is not known for the life cycle of T. cruzi, our work provides new tools for further investigations of factors connected with this protozoan pathogen infection.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Trypanosoma cruzi / Anidrases Carbônicas / Aminas / Aminoácidos Limite: Humans Idioma: En Ano de publicação: 2018 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Trypanosoma cruzi / Anidrases Carbônicas / Aminas / Aminoácidos Limite: Humans Idioma: En Ano de publicação: 2018 Tipo de documento: Article