Literature DB >> 26191185

LY2109761 enhances cisplatin antitumor activity in ovarian cancer cells.

Yuxiu Gao1, Ning Shan2, Cheng Zhao1, Yunhai Wang1, Fuliang Xu1, Jiacun Li3, Xiaoqian Yu3, Lifeng Gao3, Zhengjun Yi1.   

Abstract

BACKGROUND AND
OBJECTIVE: Ovarian cancer is among the most lethal of all malignancies in women. While chemotherapy is the preferred treatment modality, chemoresistance severely limits treatment success. Because transforming growth factor-beta (TGF-β) could increase survival of ovarian cancer cells in the presence of cisplatin, we conducted a preclinical study of the antitumor effects of the TGF-β type I (TβRI) and type II (TβRII) kinase inhibitor LY2109761 in combination with cisplatin.
METHODS: SKOV3, OV-90 and SKOV3(DDP) cells were treated with LY2109761, and/or cisplatin, and cell viability, apoptosis mRNA and protein expression levels were then evaluated. Furthermore, the efficacy of LY2109761 combined with cisplatin was further examined in established xenograft models.
RESULTS: LY2109761 was sufficient to induce spontaneous apoptosis of ovarian cancer cells. Combination with LY2109761 significantly augmented the cytotoxicity of cisplatin in both parental and cisplatin resistant ovarian cancer cells. LY2109761 significantly increased apoptotic cell death in cisplatin-resistant cells. Combination treatment of LY2109761 and cisplatin showed antiproliferative effects and induced a greater rate of apoptosis than the sum of the single-treatment rates and promoted tumor regression in established parental and cisplatin resistant ovarian cancer xenograft models.
CONCLUSIONS: Chemotherapeutic approaches using LY2109761 might enhance the treatment benefit of the cisplatin in the treatment of ovarian cancer patients.

Entities:  

Keywords:  LY2109761; Ovarian cancer; chemotherapy; transforming growth factor-beta

Mesh:

Substances:

Year:  2015        PMID: 26191185      PMCID: PMC4503057     

Source DB:  PubMed          Journal:  Int J Clin Exp Pathol        ISSN: 1936-2625


  45 in total

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