肺腺癌治療的標靶藥物開發

To overcome the current drug-resistant problems in clinical treatments of cancer patients using EGFR inhibitors, we will apply a new approach to suppress the expression of EGFR gene. We plan to use small molecular weight inhibitors that induce and stabili

@ Introduction

Epidermal growth factor receptor (EGFR) is a receptor type tyrosine kinase that has important role in cell migration, adhesion, and proliferation. Mutations that cause hyper-activation or amplification of EGFR have been associated with many cancer type include lung adenocarcinoma, glioblastoma, head and neck cancer, and anal cancers. Current cancer treatments using tyrosine kinase inhibitors (TKIs) to inhibit EGFR activity, although effective, face rigorous challenges due to the formation of drug resistance. Thus, a new approach to overcome such a hurdle is essential. Sequence analysis of EGFR promoter has revealed two regions rich in G-residues that are capable of forming G-quadruplex structures. Formation and stabilization of G-quadruplex structures by binding ligands might interfere with the expression of EGFR thus repress EGFR level in cancer cells.