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Dithiiranylmethyloxy azaxanthone shows potent anti-tumor activity via suppression of HER2 expression and HER2-mediated signals in HER2-overexpressing breast cancer cells

Title
Dithiiranylmethyloxy azaxanthone shows potent anti-tumor activity via suppression of HER2 expression and HER2-mediated signals in HER2-overexpressing breast cancer cells
Authors
Nam J.M.Jeon K.-H.Kwon H.Lee E.Jun K.-Y.Jin Y.B.Lee Y.-S.Na Y.Kwon Y.
Ewha Authors
권영주이윤실
SCOPUS Author ID
권영주scopus; 이윤실scopus
Issue Date
2013
Journal Title
European Journal of Pharmaceutical Sciences
ISSN
0928-0987JCR Link
Citation
vol. 50, no. 2, pp. 181 - 190
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
Dithiiranylmethyloxy azaxanthone (CHO10), which was discovered by screening compounds in a reporter gene assay, inhibited the ESX-Sur2 interaction in a dose-dependent manner with potency similar to canertinib. The intervention of CHO10 during the ESX-Sur2 interaction caused down-regulation of both HER2 gene amplification and HER2 protein expression, which led to the attenuation of HER2-mediated downstream signal cascades and autocrine cell growth in SK-BR-3 cells, which are HER2 overexpressing breast cancer cells. The cell growth inhibitory activity of CHO10 was more potent in HER2-overexpressing breast cancer cells (AU-565, BT474 and SK-BR-3) than in HER2-negative cells (HEK293) and breast cancer cells (MCF-7) that express a basal level of HER2. Treatment with CHO10 in combination with tamoxifen sensitized BT474 cells, tamoxifen-resistant ER-positive breast cancer cell line, toward chemotherapeutic. The anti-tumor activity of CHO10 was validated by the significant reduction in tumor size of NCI-H460 or DLD-1 subcutaneously implanted xenograft tumors through treatment with 1 mg/kg five times every other 2 days. © 2013 Elsevier B.V.
DOI
10.1016/j.ejps.2013.06.014
Appears in Collections:
약학대학 > 약학과 > Journal papers
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