The potent protein phosphatase 2A inhibitors aminocytostatins: new derivatives of cytostatin.
J Antibiot (Tokyo)
; 74(10): 743-751, 2021 10.
Article
en En
| MEDLINE
| ID: mdl-34290381
ABSTRACT
Specific inhibitors of protein phosphatase 2A (PP2A) mediate anticancer effects by augmenting the tumor-killing activity of natural killer (NK) cells. In this study, new PP2A inhibitors, aminocytostatins A-E, were isolated from Kitasatospora sp. MJ654-NF4 and structurally characterized. Aminocytostatins are derivatives of cytostatin, which is a specific PP2A inhibitor isolated from the same organism, and aminocytostatins have a characteristic amino group within the lactone moiety. Compared to cytostatin, aminocytostatin A showed a stronger inhibitory activity against PP2A in vitro and augmented the tumor-killing activity of NK cells in vivo. Furthermore, a docking model was generated to demonstrate the favorable activities of aminocytostatin A.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Organofosfatos
/
Pironas
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Streptomycetaceae
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Proteína Fosfatasa 2
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Antineoplásicos
Tipo de estudio:
Prognostic_studies
Límite:
Animals
Idioma:
En
Año:
2021
Tipo del documento:
Article