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Métodos Terapêuticos e Terapias MTCI
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1.
Molecules ; 24(1)2019 Jan 02.
Artigo em Inglês | MEDLINE | ID: mdl-30609757

RESUMO

Small molecules containing quinone and/or oxime moieties have been found as promising anti-fungal agents. One of them is 4-AN, a recently reported potent anti-Candida compound, which inhibits the formation of hyphae, decreases the level of cellular phosphoproteome, and finally shows no toxicity towards human erythrocytes and zebrafish embryos. Here, further research on 4-AN is presented. The results revealed that the compound: (i) Kills Candida clinical isolates, including these with developed antibiotic resistance, (ii) affects mature biofilm, and (iii) moderately disrupts membrane permeability. Atomic force microscopy studies revealed a slight influence of 4-AN on the cell surface architecture. 4-AN was also shown to inhibit multiple various protein kinases, a characteristic shared by most of the ATP-competitive inhibitors. The presented compound can be used in novel strategies in the fight against candidiasis, and reversible protein phosphorylation should be taken into consideration as a target in designing these strategies.


Assuntos
Antifúngicos/farmacologia , Candida albicans/efeitos dos fármacos , Oximas/uso terapêutico , Inibidores de Proteínas Quinases/farmacologia , Quinonas/uso terapêutico , Biofilmes/efeitos dos fármacos , Transporte Biológico , Membrana Celular , Avaliação Pré-Clínica de Medicamentos , Resistência Microbiana a Medicamentos , Humanos , Testes de Sensibilidade Microbiana , Modelos Moleculares , Estrutura Molecular , Fosforilação , Ligação Proteica , Propriedades de Superfície
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