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ACS Med Chem Lett. 2010 Sep 7;1(9):454-9. doi: 10.1021/ml100146z. eCollection 2010 Dec 9.

Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.

Author information

1
Key Laboratory of Regenerative Biology and Institute of Chemical Biology, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, #190 Kaiyuan Avenue, Guangzhou Science Park, Guangzhou, China 510530 ; Zhongshan Medical School, Sun Yat-Sen University, #74 Second Zhongshan Road, Guangzhou, China 510080.
2
Key Laboratory of Regenerative Biology and Institute of Chemical Biology, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, #190 Kaiyuan Avenue, Guangzhou Science Park, Guangzhou, China 510530.
3
Zhongshan Medical School, Sun Yat-Sen University, #74 Second Zhongshan Road, Guangzhou, China 510080.

Abstract

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.

KEYWORDS:

STAT3 signaling pathway; apoptosis; cell cycle arrest; inhibitor; niclosamide

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