Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway
复制标题
鉴定氯硝柳胺为 STAT3 信号通路的新型小分子抑制剂
DOI：
10.1021/ml100146z
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发表时间：
2010-12-01
影响因子：
4.2
通讯作者：
Ding, Ke
中科院分区：
文献类型：
--
作者：
Ren, Xiaomei;Duan, Lei;Ding, Ke
抑制信号转导子和转录激活子3（STAT3）信号通路已被认为是治疗具有组成性活性的STAT3的人类癌症的新的治疗策略。在这项研究中，我们报告了FDA批准的驱虫药氯硝柳胺作为一种新的小分子抑制剂的鉴定。STAT3信号通路。该化合物有效抑制STAT3的活化和转录功能，并因此诱导具有组成性活性STAT3的癌细胞的细胞生长抑制、细胞凋亡和细胞周期停滞。我们的研究为STAT3通路抑制剂作为新型分子靶向抗癌药物的开发提供了一种新的具有水杨酰胺骨架的有前途的先导化合物。
Inhibition of the Signal transducer and activator of transcription 3 (STAT3) signaling pathway has been considered a novel therapeutic strategy to treat human cancers with constitutively active STAT3. In this study, we report the identification of niclosamide, an FDA-approved anthelmintic drug, as a new small-molecule inhibitor. of the STAT3 signaling pathway. This compound potently inhibited the activation and transcriptional function of STAT3 and consequently induced cell growth inhibition, apoptosis, and cell cycle arrest of cancer cells with constitutively active STAT3. Our study provides a new promising lead compound with a salicylic amide scaffold for the development of STAT3 pathway inhibitors as novel molecularly targeted anticancer drugs.