ReferenceID 3686

Toosendanin demonstrates promising antitumor efficacy in osteosarcoma by targeting STAT3

Oncogene

Signal transducer and activator of transcription 3(STAT3) is an emerging target for cancer therapy. In this study, we identify Toosendanin (TSN) is an effective inhibitor of STAT3, leading to the impediment of various o

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Reference Id
3686
Evidence Id
20276
Core Evidence Id
20276
Source Reference Id
660
Herb2 Reference Id
HBREF001105
Subject Paper Key
HBIN046550_28783167
Pubmed Id
28783167
Doi
10.1038/onc.2017.270
Paper Title
Toosendanin demonstrates promising antitumor efficacy in osteosarcoma by targeting STAT3
Paper Abstract
Signal transducer and activator of transcription 3(STAT3) is an emerging target for cancer therapy. In this study, we identify Toosendanin (TSN) is an effective inhibitor of STAT3, leading to the impediment of various oncogenic processes in osteosarcoma. TSN selectively inactivates phospho-STAT3 (Tyr-705); subsequent molecular docking and in vitro SPR analysis uncover TSN directly binds to the SH2 domain of STAT3. Consequently, TSN blocks STAT3 dimerization and impairs the complex formation of STAT3 and epidermal growth factor receptor (EGFR). In an animal tumor model study, TSN is well tolerated, inhibits osteosarcoma growth and metastasis. In another osteosarcoma patient-derived xenografts (PDX) model, we find TSN triggers strong inhibitory effects on patient-derived tumors. Further studies show that TSN also displays activity against other solid tumors. Our preclinical work therefore supports that TSN acts as a novel inhibitor of STAT3 that blocks tumorigenesis in ostoesarcoma.
Journal
Oncogene
Publish Year
2017
Experiment Subject
animal tumor model,osteosarcoma patient-derived xenografts (pdx) model
Experiment Type
Clinical & Animal Experiment
Phenotype Related
Blocks Tumorigenesis In Ostoesarcoma.
Paper Title Cn
Paper Title En
Toosendanin demonstrates promising antitumor efficacy in osteosarcoma by targeting STAT3
Bilingual Status
semi_complete