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DOI: 10.1055/s-0031-1282083
Natural products derived from traditional chinese medicine as novel ınhibitors of the epidermal growth factor receptor in cancer cells
The success of established anticancer drugs is frequently hampered non-sufficient tumor specificity leading to side effects and drug resistance. Oncogene products and tumor suppressors are exquisite targets developing more specific drugs with improved features. The epidermal growth factor receptor (EGFR) became an important target for drug development. However, clinical application of EGFR tyrosine kinase inhibitors resulted in resistance to EGFR-targeting drugs due to the selection of EGFR-mutated variants. This phenomenon forced the search for novel inhibitors of EGFR and downstream signaling cascades. We investigated the prognostic role of the EGFR in human tumor biopsies (lung cancer, glioblastoma, head and neck cancer) by comparative genomic hybridization and immunohistochemistry) [1–4,6] and identified phytochemicals (dicentrine, camptothecin derivatives, artesunate etc.) affecting EGFR signaling [5,7–9]. Here, we report on recent achievements in natural products derived from medicinal plants as novel inhibitors of mutated EGFR and EGFR signal transduction pathways [10].
Keywords: Cancer, EGFR, Targeted chemotherapy, Traditional Chinese medicine
References: 1. Volm et al. (2002) Br J Cancer 87: 251–7.
2. Volm et al. (2002) Clin Cancer Res 8: 1843–8.
3. Volm et al. (2004) Cancer Genomics Proteomics1: 157–66.
4. Halatsch et al. (2004)J Neurosurg 100: 523–33.
5. Efferth et al.(2004) Biochem Pharmacol 1689–1700.
6. Konkimalla et al. (2007) Expert Rev Anticancer Ther 7: 319–29.
7. Konkimalla et al. (2009) Curr Cancer Drug Targets 9: 72–80.
8. Konkimalla et al. (2010) Biochem Pharmacol 79: 1092–1099.
9. Konkimalla et al. (2010) Biochem Pharmacol 80:39–49
10. Sertel et al. (2010) Combinat Chem High Throughput Screen 13:849–54.