Periodic Reporting for period 1 - TARGETSET (Commercial feasibility of targeting the histone methyltransferase SETD8 in cancer: New chemical entities and biomarkers.)
Reporting period: 2021-07-01 to 2022-12-31
This project was focused on the preclinical development of a new class of anticancer medicines, based on the inhibition of a protein named SETD8. This protein had been found to be altered in several tumors, and previous data suggested that molecules that could inhibit its function could be useful for the treatment of cancer, particularly certain targets of pediatric tumors such as medulloblastoma. However, the inhibitors available were very poor, and many important questions about this novel therapy still remained to be answered such as: which types of cancers would mostly benefit from this treatment? Will the patients become resistant to the treatment and how? In this context, our ERC PoC project focused on the development of novel SETD8 inhibitors with better properties than existing ones, and in addressing the above-mentioned questions about their use in cancer. In addition, we dedicated part of our activities to explore a potential commercialisation and exploitation route for our assets. The project has been successful in all its aims, and at this point we have a competitive preclinical package on a new class of early stage SETD8 inhibitors and associated knowhow, which is ready for the next steps of technology transfer with the ultimate goal of providing medical oncologists with a new weapon for the treatment of cancer.