Development of small molecule inhibitors targeting the N-terminal domain of human androgen receptor

Background The failure to help CRPC patients has created an urgent need to explore new treatments with nonconventional mechanisms of drug action. Although other signalling pathways and co-factors influence PCa progression, the androgen receptor (AR) remains as the master regulator of tumor promoting genes, representing the most credential target in both PCa and CRPC. The search for new small molecule inhibitors that target alternative pocket sites and surface exposed regions of the AR has intensified in recent years.