Nesterova, Irina V.
M.S. (Master of Science)
Department of Chemistry and Biochemistry
One of the most successful and fastest growing groups of kinase inhibitors are small molecules that compete with ATP binding. Kinase function is closely related to many diseases, specifically cancer. Kinases within living cells are essential elements in signaling cascades and post-translational modifications. However, actual kinase activity and the efficacy of its inhibitors in living systems are hard to evaluate. A way to assess inhibitor activity is through cellular assays that directly report the inhibitor’s engagement in native environments. Our goal is to develop a simple near-infrared (NIR) fluorescent HTS-compatible cellular assay for kinase inhibitor profiling in native cellular environments. By doing so, we accurately profile inhibitor candidates and minimize the failure of drug candidates because it eliminates early drug failures. The approach also personalizes the therapeutic pathways by evaluating the responses to drugs in cells derived from actual tumors. In this project, we focus on the epidermal growth factor receptor (EGFR) tyrosine kinase. EGFR is a well-established target for anticancer drug development. Our sensing system aims to profile the activity of ATP pocket binding inhibitors in native cells via a simple fluorescence-based assay.
Mohamed, Myar, "Fluorescent Cellular assays For Kinase inhibitors" (2022). Graduate Research Theses & Dissertations. 7459.
Northern Illinois University
Rights Statement 2
NIU theses are protected by copyright. They may be viewed from Huskie Commons for any purpose, but reproduction or distribution in any format is prohibited without the written permission of the authors.