Author (Your Name)

Ryan Weeks, Colby CollegeFollow

Date of Award

2016

Document Type

Honors Thesis (Open Access)

Department

Colby College. Chemistry Dept.

Advisor(s)

Kevin Rice

Second Advisor

Julie Millard

Abstract

Laromustine is a chemotherapeutic sulfonylhydrazine prodrug used in clinical trials to treat acute myeloid leukemia (AML) and glioblastoma multiforme (GBM). While treatment of AML with laromustine has more demonstrative clinical success, there are enough promising data against GBM to pursue additional pre-clinical and clinical experiments. To determine the synergistic effects caused by treating cultured GBM cells with laromustine and a library of FDA-approved compounds, a chemical genetic screen was developed. To optimize the screen, optimal cultured GBM cell seed density, growth period and maximum well capacity were determined. The treatment period for a lethal dose of laromustine in cultured GBM cells was found to be 6 hours; causing acute cell death in half as much time as the treatment with a lethal dose of Temozolomide, the current GBM treatment. The LD50 for laromustine in cultured GBM cells was observed to be approximately 700 μM when treated for 6 hours. Using these standards of optimization for maximum reproducibility, a chemical genetic screen will be used to determine the synergistic effects of laromustine with a library of characterized small molecules.

Keywords

laromustine, temozolomide, glioblastoma multiforme, chemical genetic screen

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