Project description
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.
Objective
Within our ERC CoG grant, RSHEALTH, our group has contributed to the to the preclinical development of chemical inhibitors of the ATR kinase as anticancer agents, that are now in clinical trials by several companies. During the course of our investigations, we also made important advances in developing inhibitors of SETD8, another interesting cancer-related target. SETD8 is a histone methyltransferase known to play important roles in DNA replication and repair. Evidence indicating that targeting SETD8 could be interesting for cancer therapy has been building up in recent years. For instance, SETD8 is overexpressed in a wide range of cancers, and recent works identified SETD8 as a specific vulnerability in High-Risk Neuroblastoma or MYC-driven Medulloblastomas. Unfortunately, all available SETD8 inhibitors have low potency and poor pharmacological properties, and none has progressed to the clinic. We here propose to capitalize in our strengths in academic drug development, and our experience in transferring our inhibitors to the industry, in order to facilitate the clinical development SETD8 inhibitors. Our proposal includes objectives that will help us improve the quality of our inhibitors, valorise them in preclinical cancer models and develop companion biomarkers that would be used for patient stratification. All of this would be integrated within a business plan that should facilitate a coherent development of this line of work oriented towards the clinical development of SETD8 inhibitors for the benefit of cancer patients.
Fields of science (EuroSciVoc)
CORDIS classifies projects with EuroSciVoc, a multilingual taxonomy of fields of science, through a semi-automatic process based on NLP techniques. See: The European Science Vocabulary.
CORDIS classifies projects with EuroSciVoc, a multilingual taxonomy of fields of science, through a semi-automatic process based on NLP techniques. See: The European Science Vocabulary.
- medical and health sciences basic medicine pharmacology and pharmacy drug discovery
- natural sciences biological sciences genetics DNA
- medical and health sciences clinical medicine oncology
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Keywords
Project’s keywords as indicated by the project coordinator. Not to be confused with the EuroSciVoc taxonomy (Fields of science)
Project’s keywords as indicated by the project coordinator. Not to be confused with the EuroSciVoc taxonomy (Fields of science)
Programme(s)
Multi-annual funding programmes that define the EU’s priorities for research and innovation.
Multi-annual funding programmes that define the EU’s priorities for research and innovation.
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H2020-EU.1.1. - EXCELLENT SCIENCE - European Research Council (ERC)
MAIN PROGRAMME
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Topic(s)
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Calls for proposals are divided into topics. A topic defines a specific subject or area for which applicants can submit proposals. The description of a topic comprises its specific scope and the expected impact of the funded project.
Funding Scheme
Funding scheme (or “Type of Action”) inside a programme with common features. It specifies: the scope of what is funded; the reimbursement rate; specific evaluation criteria to qualify for funding; and the use of simplified forms of costs like lump sums.
Funding scheme (or “Type of Action”) inside a programme with common features. It specifies: the scope of what is funded; the reimbursement rate; specific evaluation criteria to qualify for funding; and the use of simplified forms of costs like lump sums.
ERC-POC - Proof of Concept Grant
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Call for proposal
Procedure for inviting applicants to submit project proposals, with the aim of receiving EU funding.
Procedure for inviting applicants to submit project proposals, with the aim of receiving EU funding.
(opens in new window) ERC-2020-PoC
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Net EU financial contribution. The sum of money that the participant receives, deducted by the EU contribution to its linked third party. It considers the distribution of the EU financial contribution between direct beneficiaries of the project and other types of participants, like third-party participants.
28029 Madrid
Spain
The total costs incurred by this organisation to participate in the project, including direct and indirect costs. This amount is a subset of the overall project budget.