Determining the Relative Binding Efficacy of Selective Estrogen Receptor Modulators

Abstract

Breast cancer is the second leading cause of breast cancer death among women in the United States, which highlights the importance of broadening breast cancer drug development and research. Treatment for those with breast cancer can be determined by biomarkers and the subtype of breast cancer, which presents the obstacle of subtypes and affiliated resistance for breast cancer drug development. Our lab focused on maximizing the effectiveness of estrogen-receptor positive breast cancer drugs by testing a new fluorophore in conjunction with both new and old breast cancer drugs. Fluorescence anisotropy was then used to test the binding affinity of various estrogen receptor-targeted compounds in order to determine their relative binding efficacies and compare them to those found in past studies using a different fluorophore. We found that the novel fluorophore coumestrol can be used effectively in the estrogen receptor binding assay and that Weatherman-made compounds generated data that would suggest the potential for further study as breast cancer drugs.