Antitumor activity of a novel PARP1/2 inhibitor YHP-743 / 药学学报
Acta Pharmaceutica Sinica
; (12): 938-943, 2018.
Article
em Zh
| WPRIM
| ID: wpr-779954
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WPRO
ABSTRACT
Poly(ADP-ribose) polymerase (PARP)-1 and PARP2 function as ADP-ribosylases involved in DNA repair. PARP1/2 is highly expressed in cancers and emerged as an attractive target for antitumor drug. In this study, we investigated the antitumor activity of a novel PARP1/2 inhibitor YHP-743 in vitro and in vivo. The results showed that YHP-743 had potent enzymatic inhibitory activity against PARP1 and PARP2 to down-regulate the PAR level. YHP-743 not only inhibited breast cancer cells with genes deficiency of homologous recombination repair, but also potentiated chemotherapy agent's cytotoxicity, such as temozolomide, topotecan, cisplatin and doxorubicin. YHP-743 elicited good antitumor activity in combination with temo-zolomide in vivo.
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WPRIM
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2018
Tipo de documento:
Article