Research Interest
Androgen Receptor Activity
The androgen receptor (AR) is a nuclear receptor transcription factor important in the development and progression of prostate cancer, including aggressive hormone-refractory tumours. Activated AR binds to androgen-responsive elements in DNA to promote gene transcription. Our collaborator Dr Michelle Garrett has carried out a cell-based screen for inhibitors of AR transcriptional function, from which two distinct series of inhibitors were identified.
The aim of the project is to apply chemical proteomic techniques to identify the molecular target(s) of these compounds and to assess if these are novel druggable targets for inhibiting AR signalling in prostate cancer. We are using the ‘bait and hook’ approach developed by Hatanaka and others that combines affinity probes with photolabelling. The covalent photolabelling of targets facilitates the isolation and identification of the target proteins, and can also provide information on the sites of binding of the hit compounds.