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- W2000711256 abstract "Over-activation of ErbB2 highly correlates with tumor progression and chemoresistance and has become an important biomarker and major target of cancer therapy treatments. Although several chemotherapy agents targeting ErbB2 show promising therapeutic effect, additional therapeutic approaches targeting ErbB2 are still urgently needed. Emodin, a major anthraquinone in the rhizome of Rheum palmatum, has been demonstrated to exhibit anticancer effects on several human ErbB2-overexpressing cancers. Computer modeling analysis determined emodin could be a suitable fit for the ErbB2 active pocket site however, the initial binding was unsatisfactory. In order to improve the anti-ErbB2 activity, a series of emodin analogs were synthesized and evaluated against several ErbB2-overexpressing oral cancer cells. Among them, 1,8-dihydroxy-9(10H)-anthraquinone (Em08red), showed potent antiproliferative effect against ErbB2-overexpessing oral cancers. Further studies showed Em08red treatment significantly reduced the levels of ErbB2 phosphorylation, resulting in G2/M arrested and apoptotic cell death. Moreover, treatment with Em08red, significant reduced the levels of anti-apoptosis proteins (Bcl-x and Bcl-2) and activated the caspase-3 and -9, but not caspase-8. Collectively, our results clearly indicate Em08red can down-regulate ErbB2-signaling, induce intrinsic apoptotic cell death and is a promising potent ErbB2-targeted therapeutic. Citation Information: Mol Cancer Ther 2013;12(11 Suppl):C116. Citation Format: Shin-Hun P. Juang, Fong-Pin Liang, Jin-Chern Lien, Yu-Hwa Wu, Chien-Shu Chen. Em08red, an emodin analog, exhibited anti-proliferative activity against oral cancer through down-regulation of ErbB2 signaling pathway and induction of apoptosis. [abstract]. In: Proceedings of the AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics; 2013 Oct 19-23; Boston, MA. Philadelphia (PA): AACR; Mol Cancer Ther 2013;12(11 Suppl):Abstract nr C116." @default.
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- W2000711256 date "2013-11-01" @default.
- W2000711256 modified "2023-09-25" @default.
- W2000711256 title "Abstract C116: Em08red, an emodin analog, exhibited anti-proliferative activity against oral cancer through down-regulation of ErbB2 signaling pathway and induction of apoptosis." @default.
- W2000711256 doi "https://doi.org/10.1158/1535-7163.targ-13-c116" @default.
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