ReferenceID 5967
Periplogenin suppresses the growth of esophageal squamous cell carcinoma in vitro and in vivo by targeting STAT3
Oncogene
The mortality rate of esophageal squamous cell carcinoma (ESCC) is higher than that of other cancers worldwide owing to a lack of therapeutic targets and related drugs. This study aimed to find new drugs by targeting an
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Record Fields
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- Reference Id
- 5967
- Evidence Id
- 22557
- Core Evidence Id
- 22557
- Source Reference Id
- 5196
- Herb2 Reference Id
- HBREF005993
- Subject Paper Key
- HBIN039283_33986510
- Pubmed Id
- 33986510
- Doi
- 10.1038/s41388-021-01817-2
- Paper Title
- Periplogenin suppresses the growth of esophageal squamous cell carcinoma in vitro and in vivo by targeting STAT3
- Paper Abstract
- The mortality rate of esophageal squamous cell carcinoma (ESCC) is higher than that of other cancers worldwide owing to a lack of therapeutic targets and related drugs. This study aimed to find new drugs by targeting an efficacious therapeutic target in ESCC patients. Signal transducer and activator of transcription 3 (STAT3) is hyperactive in ESCC. Herein, we identified a novel STAT3 inhibitor, periplogenin, which strongly inhibited phosphorylation of STAT3 at Tyr705. Docking models and pull-down assays revealed that periplogenin bound directly and specifically to STAT3, leading to significant suppression of subsequent dimerization, nuclear import, and transcription activities. In addition, STAT3 knockdown cell lines were insensitive to periplogenin, whereas in contrast, STAT3-overexpressing cells were more sensitive to periplogenin, indicating that STAT3 was a target of periplogenin. Intraperitoneally administered periplogenin exhibited efficacious therapeutic effects in ESCC patient-derived xenograft models and dramatically impaired the phosphorylation of STAT3 and expression levels of STAT3-mediated downstream genes. Thus, our study demonstrated that periplogenin acted as a new STAT3 inhibitor, suppressing the growth of ESCC in vitro and in vivo, providing a basis for its potential application in ESCC treatment and prevention.
- Journal
- Oncogene
- Publish Year
- 2021
- Experiment Subject
- patient; stat3 knockdown cell lines
- Experiment Type
- Cell Experiment
- Phenotype Related
- Cancers; Esophageal Squamous Cell Carcinoma
- Paper Title Cn
- Paper Title En
- Periplogenin suppresses the growth of esophageal squamous cell carcinoma in vitro and in vivo by targeting STAT3
- Bilingual Status
- semi_complete