Canberra's world-first trial targets 'undruggable' cancer

Canberra's world-first trial targets 'undruggable' cancer

ANU Professor Mark Polizzotto heads up a world-first cancer trial. Photo: Jack Fox/ANU. Some researchers refer to MYC-driven cancers as notorious and infamous. They’re difficult to treat and aggressive, and attempts to treat them by inhibiting the MYC gene have stalled in the past. But now a world-first trial in Canberra will target the infamous “undruggable” cancer gene with a newly developed MYC inhibitor drug – PMR-116. Leading the trial, Aus…

From “undruggable” target to clinical potential: The journey of AOH1996 - The Cancer Letter

When I first proposed targeting PCNA (proliferating cell nuclear antigen) as a therapeutic approach, the response I got was: “No one will ever make a drug against PCNA. It’s undruggable.” The protein lacks enzymatic activity, has a disordered region, and binds to over 200 other proteins within the cell. From a traditional drug development perspective, these characteristics made PCNA an impossible target. Yet sometimes the most challenging proble…