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Nifuratel, a novel STAT3 inhibitor with potent activity against human gastric cancer cells.
Cancer Management and Research ( IF 2.5 ) Pub Date : 2017-11-16 , DOI: 10.2147/cmar.s146173
Hailun Zheng 1, 2 , Huang Hong 1 , Lulu Zhang 1, 2 , Xiong Cai 1, 2 , Meng Hu 1, 2 , Yuepiao Cai 2 , Bin Zhou 1 , Jiayuh Lin 3 , Chengguang Zhao 2 , Wanle Hu 1
Affiliation  

Activation of the signal transducer and activator of transcription 3 (STAT3) is observed in multiple cancer types, including gastric cancer, and represents a potential drug target for chemotherapy. Currently, clinically available small-molecule inhibitors targeting STAT3 are lacking. Here, we report that nifuratel, an antiprotozoal and antifungal drug, is a potent inhibitor of STAT3. We found that nifuratel significantly suppressed proliferation and induced apoptosis of gastric cancer cells. Studies of the mechanism of action of nifuratel indicated that it acts by inhibiting the constitutive and interleukin-6-induced STAT3 activation. Taken together, our findings demonstrate that nifuratel may be a novel, clinically accessible STAT3 inhibitor in gastric cancer cells.

中文翻译:

Nifuratel,一种新型的STAT3抑制剂,对人胃癌细胞具有有效活性。

在包括胃癌在内的多种癌症类型中观察到信号转导子和转录激活子3(STAT3)的激活,代表了化学疗法的潜在药物靶标。当前,缺乏靶向STAT3的临床上可用的小分子抑制剂。在这里,我们报道硝呋太尔是一种抗原生动物和抗真菌药物,是STAT3的有效抑制剂。我们发现硝呋太尔显着抑制胃癌细胞的增殖并诱导其凋亡。对硝呋太尔作用机理的研究表明,它通过抑制组成型和白介素6诱导的STAT3激活而起作用。综上所述,我们的发现表明硝呋太尔可能是胃癌细胞中一种新型的,临床上可使用的STAT3抑制剂。
更新日期:2019-11-01
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