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

Xiaomei Ren(Guangzhou Institutes of Biomedicine and Health), Lei Duan(Guangzhou Institutes of Biomedicine and Health), Qiang He(Guangzhou Institutes of Biomedicine and Health), Zhang Zhang(Guangzhou Institutes of Biomedicine and Health), Yi Zhou(Guangzhou Institutes of Biomedicine and Health), Donghai Wu(Guangzhou Institutes of Biomedicine and Health), Jingxuan Pan(Sun Yat-sen University), Duanqing Pei(Guangzhou Institutes of Biomedicine and Health), Ke Ding(Guangzhou Institutes of Biomedicine and Health)
ACS Medicinal Chemistry Letters
September 7, 2010
Cited by 230Open Access
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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.


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