Clinical development of SETD8 inhibitors
Work in the ERC-funded project RSHEALTH has made significant progress in developing inhibitors of SETD8, a histone methyltransferase. Overexpressed in several cancers, it plays significant roles in DNA replication and repair. However, all available SETD8 inhibitors have low potency and poor pharmacological characteristics, and none have progressed to the clinic. At the same time, recent research identified SETD8 as a specific vulnerability in high-risk neuroblastoma and MYC-driven medulloblastomas. The EU-funded TARGETSET project will build on RSHEALTH results and the experience of transferring the inhibitors to the industry, facilitating the clinical development of SETD8 inhibitors. The project will improve inhibitors’ quality, valorise them in preclinical cancer models and develop companion biomarkers for patient stratification.
Fields of science
Funding SchemeERC-POC-LS - ERC Proof of Concept Lump Sum Pilot
See on map