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Antitumor activity of HM781-36B, a pan-HER tyrosine kinase inhibitor, in HER2-amplified breast cancer cells
DC Field | Value | Language |
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dc.contributor.author | Kim, Hye Jin | - |
dc.contributor.author | Kim, Hwang-Phill | - |
dc.contributor.author | Yoon, Young-Kwang | - |
dc.contributor.author | Kim, Maeng-Sup | - |
dc.contributor.author | Lee, Gwan-Sun | - |
dc.contributor.author | Han, Sae-Won | - |
dc.contributor.author | Im, Seock-Ah | - |
dc.contributor.author | Kim, Tae-You | - |
dc.contributor.author | Oh, Do-Youn | - |
dc.contributor.author | Bang, Yung-Jue | - |
dc.date.accessioned | 2021-01-31T11:00:46Z | - |
dc.date.available | 2021-01-31T11:00:46Z | - |
dc.date.created | 2020-08-27 | - |
dc.date.created | 2020-08-27 | - |
dc.date.created | 2020-08-27 | - |
dc.date.created | 2020-08-27 | - |
dc.date.created | 2020-08-27 | - |
dc.date.issued | 2012-03 | - |
dc.identifier.citation | Anti-Cancer Drugs, Vol.23 No.3, pp.288-297 | - |
dc.identifier.issn | 0959-4973 | - |
dc.identifier.other | 112024 | - |
dc.identifier.uri | https://hdl.handle.net/10371/172962 | - |
dc.description.abstract | HM781-36B is an orally administered pan-human epidermal growth factor receptor (HER) inhibitor. To explore the role of pan-HER inhibitor in breast cancer, we investigated the antitumor effect and mechanisms of HM781-36B in breast cancer cell lines. Six breast cancer cell lines (BT474, MDA-MB-453, SK-BR-3, T47D, MCF-7, and MDA-MB-231) were tested. The growth inhibitory effect was assessed using the tetrazolium bromide [3-(4,5-dimethylthiazole-2-yl)-2,5-diphenyl-tetrazolium bromide] assay. The cell cycle at various concentrations of HM781-36B was analyzed by flow cytometry, and analysis of downstream molecules was performed by western blot analysis. Interaction of HM781-36B with cytotoxic chemotherapeutic agents was analyzed by combination index using CalcuSyn. The HER2-amplified cells (SK-BR-3, BT474, and MDA-MB-453) were sensitive to HM781-36B (IC50 = 0.001 mu mol/l, 0.0012 mu mol/l, and 0.0095 mu mol/l, respectively). HM781-36B induced G1 arrest and resulted in apoptosis. It reduced the level of p-HER2, p-AKT, p-ERK, and p-STAT3. HM781-36B combined with 5-fluorouracil, cisplatin, paclitaxel, or gemcitabine showed a synergistic inhibitory effect on the HER2-amplified and on some of the HER2-nonamplified breast cancer cells. HM781-36B could be a promising treatment for HER2-amplified breast cancer as a single agent or in combination with cytotoxic agents and can be a candidate for treatment of HER2-nonamplified breast cancer in combination with cytotoxic agents. Anti-Cancer Drugs 23: 288-297 (C) 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins. | - |
dc.language | 영어 | - |
dc.publisher | Lippincott Williams & Wilkins Ltd. | - |
dc.title | Antitumor activity of HM781-36B, a pan-HER tyrosine kinase inhibitor, in HER2-amplified breast cancer cells | - |
dc.type | Article | - |
dc.contributor.AlternativeAuthor | 임석아 | - |
dc.identifier.doi | 10.1097/CAD.0b013e32834e7d9b | - |
dc.citation.journaltitle | Anti-Cancer Drugs | - |
dc.identifier.wosid | 000300278900005 | - |
dc.identifier.scopusid | 2-s2.0-84863274596 | - |
dc.citation.endpage | 297 | - |
dc.citation.number | 3 | - |
dc.citation.startpage | 288 | - |
dc.citation.volume | 23 | - |
dc.identifier.sci | 000300278900005 | - |
dc.description.isOpenAccess | N | - |
dc.contributor.affiliatedAuthor | Im, Seock-Ah | - |
dc.contributor.affiliatedAuthor | Kim, Tae-You | - |
dc.contributor.affiliatedAuthor | Oh, Do-Youn | - |
dc.contributor.affiliatedAuthor | Bang, Yung-Jue | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.subject.keywordPlus | LAPATINIB RESISTANCE | - |
dc.subject.keywordPlus | LUNG-CANCER | - |
dc.subject.keywordPlus | PHASE-II | - |
dc.subject.keywordPlus | TRASTUZUMAB RESISTANCE | - |
dc.subject.keywordPlus | ADJUVANT CHEMOTHERAPY | - |
dc.subject.keywordPlus | MONOCLONAL-ANTIBODY | - |
dc.subject.keywordPlus | RECEPTOR INHIBITOR | - |
dc.subject.keywordPlus | GASTRIC-CANCER | - |
dc.subject.keywordPlus | SOLID TUMORS | - |
dc.subject.keywordPlus | ACTIVATION | - |
dc.subject.keywordAuthor | breast cancer | - |
dc.subject.keywordAuthor | HM781-36B | - |
dc.subject.keywordAuthor | pan-HER inhibitor | - |
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