ReferenceID 5299
Genipin suppression of growth and metastasis in hepatocellular carcinoma through blocking activation of STAT-3
J Exp Clin Cancer Res
BACKGROUND: The signal transducer and activator of transcription-3 (STAT-3) can facilitate cancer progression and metastasis by being constitutively active via various signaling. Abundant evidence has indicated that STAT
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Record Fields
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- Reference Id
- 5299
- Evidence Id
- 21889
- Core Evidence Id
- 21889
- Source Reference Id
- 3856
- Herb2 Reference Id
- HBREF004653
- Subject Paper Key
- HBIN027445_32741371
- Pubmed Id
- 32741371
- Doi
- 10.1186/s13046-020-01654-3
- Paper Title
- Genipin suppression of growth and metastasis in hepatocellular carcinoma through blocking activation of STAT-3
- Paper Abstract
- BACKGROUND: The signal transducer and activator of transcription-3 (STAT-3) can facilitate cancer progression and metastasis by being constitutively active via various signaling. Abundant evidence has indicated that STAT-3 may be a promising molecular target for cancer treatment. METHODS: In this study, a dual-luciferase assay-based screening of 537 compounds for STAT-3 inhibitors of hepatocellular carcinoma (HCC) cells was conducted, leading to the identification of genipin. Effects of genipin on HCC were assessed in a patient-derived xenograft nude mice model. Western blotting assay, chromatin immunoprecipitation (ChIP) assay, molecular docking study, tube formation assay, three-dimensional top culture assay, histological examination, and immunofluorescence were utilized to evaluate the regulatory signaling pathway. RESULTS: Our research demonstrated that genipin suppresses STAT-3 phosphorylation and nuclear translocation, which may be attributed to the binding capacity of this compound to the Src homology-2 (SH2) domain of STAT-3. In addition, the therapeutic effects of genipin in a patient-derived HCC xenograft nude mice model were also demonstrated. CONCLUSIONS: In conclusion, genipin showed therapeutic potential for HCC treatment by interacting with the SH2-STAT-3 domain and suppressing the activity of STAT-3. In the future, further research is planned to explore the potential role of genipin in combination with chemotherapy or radiotherapy for HCC.
- Journal
- J Exp Clin Cancer Res
- Publish Year
- 2020
- Experiment Subject
- mouse; patient
- Experiment Type
- Animal & Cell Experiment
- Phenotype Related
- Cancer; Hepatocellular Carcinoma
- Paper Title Cn
- Paper Title En
- Genipin suppression of growth and metastasis in hepatocellular carcinoma through blocking activation of STAT-3
- Bilingual Status
- semi_complete