ARtin. New inhibitors to treat castration-resistant prostate cancer
Fundació Institut de Recerca Biomèdica, Barcelona, Spain
Prostate cancer (PC) is the second leading cause of male cancer mortality. Tumour growth depends on the activity of the androgen receptor (AR), a transcription factor activated by androgens. 30% of PC patients become refractory to current therapies targeting the hormone binding domain of AR and reach a stage of the disease known as castration resistant prostate cancer (CRPC). CRPC currently has no cure and developing therapies to fight it is of paramount importance.
ARtin aims to find inhibitors of the activation domain of the androgen receptor, until recently considered “undruggable”. This domain is indispensable for AR transactivation and is validated as a CRPC target. Our innovative approach is based on a state-of-the-art assay that allowed the identification of very potent AR inhibitors.
A novel screening method has been developing to identify several families of molecules that act upon AR with a disruptive mechanism of action. These compounds are very potent in cellular assays and are therefore promising candidates for CRPC drugs.