A small molecule inhibitor of p53-inducible protein phosphatase PPM1D.
Bioorg Med Chem Lett
; 22(1): 729-32, 2012 Jan 01.
Article
en En
| MEDLINE
| ID: mdl-22115592
ABSTRACT
PPM1D is a p53-inducible Ser/Thr protein phosphatase. PPM1D gene amplification and overexpression have been reported in a variety of human tumors, including breast cancer and neuroblastoma. Because the phosphatase activity of PPM1D is essential for its oncogenic role, PPM1D inhibitors should be viable anti-cancer agents. In our current study, we showed that SPI-001 was a potent and specific PPM1D inhibitor. SPI-001 inhibited PPM1D phosphatase activity in PPM1D-overexpressing human breast cancer cells and increased phosphorylation of p53. Furthermore, SPI-001 suppressed cell proliferation by inducing apoptosis. Our present study suggested that SPI-001 was a potential lead compound in developing anti-cancer drugs.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Fenantrenos
/
Proteína p53 Supresora de Tumor
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Fosfoproteínas Fosfatasas
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Neoplasias
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2012
Tipo del documento:
Article
País de afiliación:
Japón