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Acta Biochim Pol ; 67(2): 219-223, 2020 Jun 18.
Artículo en Inglés | MEDLINE | ID: mdl-32559055

RESUMEN

Small protein tyrosine phosphatase (PtpA) of Mycobacterium tuberculosis is attributed to the development of latent tuberculosis infection, and hence bocomes an interesting target for drug development. In this communication, inhibition of PtpA by naturally occurring fatty acids cis-2 and trans-2-eicosenoic acid is investigated. Mtb PtpA was heterologously expressed in Escherichia coli, and the activity of PtpA was inhibited by cis-2 and trans-2 eicosenoic fatty acids. Both compunds showed strong inhibition of PtpA activity with IC50 at low micromolar concentration. As comparison, trans-11-eicosenoic acid only slightly inhibit PtpA. In silico analysis confirmed the inhibition of PtpB by cis-2-eicosenoic acid by formation of several hydrogen bonds. These findings show that cis-2 and trans-2 eicosenoic fatty acids are potential candidates for latent tuberculosis inhibitors.


Asunto(s)
Proteínas Bacterianas/antagonistas & inhibidores , Proteínas Bacterianas/metabolismo , Descubrimiento de Drogas/métodos , Ácidos Grasos Monoinsaturados/metabolismo , Ácidos Grasos Monoinsaturados/farmacología , Mycobacterium tuberculosis/enzimología , Proteínas Tirosina Fosfatasas/antagonistas & inhibidores , Proteínas Tirosina Fosfatasas/metabolismo , Ácidos Grasos trans/metabolismo , Ácidos Grasos trans/farmacología , Escherichia coli/genética , Escherichia coli/metabolismo , Enlace de Hidrógeno , Concentración 50 Inhibidora , Tuberculosis Latente/tratamiento farmacológico , Tuberculosis Latente/microbiología , Ligandos , Simulación del Acoplamiento Molecular
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