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C188-9, a small-molecule STAT3 inhibitor, exerts an antitumor effect on head and neck squamous cell carcinoma.

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Abnormal activation of signal transducer and activator of transcription 3 (STAT3) is complicated in the tumor progression of multiple cancers including human head and neck squamous cell carcinoma (HNSCC) and,… Click to show full abstract

Abnormal activation of signal transducer and activator of transcription 3 (STAT3) is complicated in the tumor progression of multiple cancers including human head and neck squamous cell carcinoma (HNSCC) and, therefore, serves as a potent therapeutic target. In this study, we identify that C188-9, a small-molecule STAT3 inhibitor, exhibits an antitumor effect on HNSCC in vitro. C188-9 significantly inhibits cell growth, arrests cell cycle at G0/G1 phase, and induces apoptosis in HNSCC. Besides, the capacities of migration and invasion of HNSCC cells are impaired with the exposure to C188-9. In addition, C188-9 treatment enhanced the chemosensitivity of HNSCC cells in vitro. Moreover, C188-9 inactivates STAT3 by reducing its phosphorylation at Tyr705. Taken together, these results indicate that C188-9 could be a promising therapeutic strategy for patients suffered from HNSCC by suppressing the STAT3 pathway.

Keywords: stat3; neck squamous; squamous cell; c188; head neck

Journal Title: Anti-Cancer Drugs
Year Published: 2019

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