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dc.contributor.authorHong, Ming
dc.contributor.authorLee, Selena
dc.contributor.authorClayton, Jacob
dc.contributor.authorYake, Wildman
dc.contributor.authorLi, Jinke
dc.identifier.citationHong, M., Lee, S., Clayton, J., Yake, W., & Li, J. (2020). Genipin suppression of growth and metastasis in hepatocellular carcinoma through blocking activation of STAT-3. Journal of experimental & clinical cancer research : CR, 39(1), 146.
dc.descriptionThis work is licensed under a Creative Commons Attribution 4.0 International License.en_US
dc.description.abstractBackground 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.
dc.description.sponsorshipXing-lin Foundation (GZF-1366732 K)en_US
dc.description.sponsorshipNIH NS79432en_US
dc.rightsCopyright © 2020, The Author(s)en_US
dc.titleGenipin suppression of growth and metastasis in hepatocellular carcinoma through blocking activation of STAT-3en_US
kusw.kuauthorHong, Ming
kusw.kuauthorLee, Selena
kusw.kuauthorClayton, Jacob
kusw.kuauthorYake, Wildman
kusw.kuauthorLi, Jinke
kusw.kudepartmentPharmacology & Toxicologyen_US
kusw.oaversionScholarly/refereed, publisher versionen_US
kusw.oapolicyThis item meets KU Open Access policy criteria.en_US

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