[PMID]: | 29231751 |
[Au] Autor: | Angeli A; Del Prete S; Osman SM; Alasmary FAS; AlOthman Z; Donald WA; Capasso C; Supuran CT |
[Ad] Endereço: | a Dipartimento Neurofarba, Sezione di Scienze Farmaceutiche e Nutraceutiche , Università degli Studi di Firenze , Florence , Italy. |
[Ti] Título: | Activation studies of the α- and ß-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae with amines and amino acids. |
[So] Source: | J Enzyme Inhib Med Chem;33(1):227-233, 2018 Dec. |
[Is] ISSN: | 1475-6374 |
[Cp] País de publicação: | England |
[La] Idioma: | eng |
[Ab] Resumo: | The α- and ß-class carbonic anhydrases (CAs, EC 4.2.1.1) from the pathogenic bacterium Vibrio cholerae, VchCAα, and VchCAß, were investigated for their activation with natural and non-natural amino acids and amines. The most effective VchCAα activators were L-tyrosine, histamine, serotonin, and 4-aminoethyl-morpholine, which had K s in the range of 8.21-12.0 µM. The most effective VchCAß activators were D-tyrosine, dopamine, serotonin, 2-pyridyl-methylamine, 2-aminoethylpyridine, and 2-aminoethylpiperazine, which had K s in the submicromolar - low micromolar range (0.18-1.37 µM). The two bacterial enzymes had very different activation profiles with these compounds, between each other, and in comparison to the human isoforms hCA I and II. Some amines were selective activators of VchCAß, including 2-pyridylmethylamine (K of 180 nm for VchCAß, and more than 20 µM for VchCAα and hCA I/II). The activation of CAs from bacteria, such as VchCAα/ß has not been considered previously for possible biomedical applications. It would be of interest to study in more detail the extent that CA activators are implicated in the virulence and colonisation of the host by such pathogenic bacteria, which for Vibrio cholerae, is highly dependent on the bicarbonate concentration and pH in the surrounding tissue. |
[Mh] Termos MeSH primário: |
Aminas/farmacologia Aminoácidos/farmacologia Inibidores da Anidrase Carbônica/farmacologia Anidrases Carbônicas/metabolismo Vibrio cholerae/enzimologia
|
[Mh] Termos MeSH secundário: |
Aminas/síntese química Aminas/química Aminoácidos/síntese química Aminoácidos/química Inibidores da Anidrase Carbônica/síntese química Inibidores da Anidrase Carbônica/química Relação Dose-Resposta a Droga Seres Humanos Estrutura Molecular Relação Estrutura-Atividade Vibrio cholerae/patogenicidade
|
[Pt] Tipo de publicação: | JOURNAL ARTICLE |
[Nm] Nome de substância:
| 0 (Amines); 0 (Amino Acids); 0 (Carbonic Anhydrase Inhibitors); EC 4.2.1.1 (Carbonic Anhydrases) |
[Em] Mês de entrada: | 1712 |
[Cu] Atualização por classe: | 171221 |
[Lr] Data última revisão:
| 171221 |
[Sb] Subgrupo de revista: | IM |
[Da] Data de entrada para processamento: | 171213 |
[St] Status: | MEDLINE |
[do] DOI: | 10.1080/14756366.2017.1412316 |
|
|