Delphinidin: A Novel Agent for Inhibition of Breast Tumor Kinase Signaling by Targeting EGFR PRINCIPAL INVESTIGATOR:

Zaman N, Afaq F, Khan N, Syed DN, and Mukhtar H. Delphinidin, a major anthocyanin in pigmented fruits and vegetables is a potent inhibitor of epidermal growth factor receptor and its downstream signaling pathway. The 97 Annual Meeting of the American Association for Cancer Research, Washington, DC, USA (April 1-5, 2006). CONCLUSIONS: This study identifies an abundant fruits and vegetables based anthocyanin delphinidin as an effective inhibitor of EGFR signaling at least in breast cancer cells that act through novel Brk signaling pathway and holds great promise for its treatment. REFERENCES: 1. Mendelsohn J and Baselga J. Status of epidermal growth factor receptor antagonists in the biology and treatment of cancer. J. Clin. Oncol., 21:2787-2799, 2003. 2. Kari C, Chan TO, Rocha de Quadros M and Rodeck U. Targeting the epidermal growth factor receptor in cancer: apoptosis takes center stage. Cancer Res., 63:1–5, 2003. 3. Gschwind A, Fischer OM and Ullrich A. The discovery of receptor tyrosine kinases: targets for cancer therapy. Nat. Rev. Cancer, 4:361-370, 2004. 4. Costa S, Stamm H, Almendral A, et al. Predictive value of EGF receptor in breast cancer. Lancet, 2:1258, 1988. 5. Chen HY, Shen CH, Tsai YT, Lin FC, Huang YP and Chen RH. Brk activates rac1 and promotes cell migration and invasion by phosphorylating paxillin. Mol. Cell. Biol., 24:10558-10572, 2004. 6. Barker KT, Jackson LE and Crompton MR. BRK tyrosine kinase expression in a high proportion of human breast carcinomas. Oncogene, 15:799-805, 1997. 7. Kamalati T, Jolin HE, Mitchell PJ, Barker KT, Jackson LE, Dean CJ, Page MJ, Gusterson BA and Crompton MR. Brk, a breast tumor-derived non-receptor proteintyrosine kinase, sensitizes mammary epithelial cells to epidermal growth factor. J. Biol. Chem., 271:30956-30963, 1996.