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Nifuratel, a novel STAT3 inhibitor with potent activity against human gastric cancer cells
Hailun Zheng1,2, Huang Hong1, Lulu Zhang1,2
1Department of Coloproctology, The Second Affiliated Hospital and Yuying Children's Hospital of Wenzhou Medical University.
Abstract:
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.
Insights
Nifuratel, an existing drug, effectively inhibits signal transducer and activator of transcription 3 (STAT3) in gastric cancer cells. This finding suggests nifuratel as a potential new chemotherapy drug for gastric cancer by blocking STAT3 activation.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Signal transducer and activator of transcription 3 (STAT3) activation is prevalent in various cancers, including gastric cancer.
- STAT3 is a promising therapeutic target for cancer chemotherapy.
- There is a lack of clinically approved small-molecule inhibitors for STAT3.
Purpose of the Study:
- To investigate nifuratel as a potential STAT3 inhibitor.
- To evaluate the efficacy of nifuratel in gastric cancer cells.
- To elucidate the mechanism of action of nifuratel on STAT3 signaling.
Main Methods:
- Assessing nifuratel's effect on gastric cancer cell proliferation and apoptosis.
- Analyzing nifuratel's impact on constitutive and interleukin-6-induced STAT3 activation.
- Investigating the molecular mechanisms underlying nifuratel's action.
Main Results:
- Nifuratel demonstrated significant suppression of gastric cancer cell proliferation.
- Nifuratel effectively induced apoptosis in gastric cancer cells.
- Nifuratel was found to inhibit both constitutive and IL-6-induced STAT3 activation.
Conclusions:
- Nifuratel is a potent inhibitor of STAT3.
- Nifuratel exhibits anti-cancer effects in gastric cancer cells.
- Nifuratel represents a potential novel, clinically accessible STAT3 inhibitor for gastric cancer treatment.
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