The finding of prevalent translocations involving the ETS transcription factors ERG and ETV1 in prostate cancer suggest they are “driver” proteins in this malignancy. However, like many important cancer genes, these transcription factors are deemed “undruggable.” The development of novel approaches to targeting such proteins would be of great interest.
Using small molecule microarrays, Nicole and her Broad colleagues identified several small molecules that appear to bind selectively to ETS factors. The ability of these compounds to inhibit ERG or ETV1 function was tested using a series of luciferase reporter assays. At least two putative binders exhibited moderate inhibitory activity.
Future studies will include evaluation of binding kinetics studies by Surface Plasmon Resonance.
PROJECT: Identification of small molecule ETS transcription factor binders
My experience at the Broad was so intense and fulfilling that I had to come back from another summer. Everyone at the Broad has been extremely supportive, and I have built relationships that will last a lifetime.