Cyclo-warhead

Project description

Over the past two decades, the pharmaceutical industry has witnessed an exponential growth in approved covalent drugs. The majority of such drugs incorporate a chemical warhead, a mild electrophilic reactive functional group that forms covalent bonds in a reversible or irreversible manner with nucleophilic aminoacid residues. The aim of this proposal is to assess the viability of a new chemical warhead in the discovery of novel kinase inhibitors.

The pharmaceutical industry has seen a surge in approved covalent drugs over the past 20 years. These drugs are designed to form stable, often irreversible bonds with specific disease targets, and rely on ‘chemical warheads’, electrophilic groups that react with amino acids in proteins, either reversibly or irreversibly. However, the effectiveness and safety of these warheads vary, necessitating the search for new options. The ERC-funded Cyclo-warhead project aims to explore a novel chemical warhead for developing kinase inhibitors – drugs that could revolutionise treatments for cancers and other diseases by targeting enzymes involved in cell growth and survival. This project could pave the way for the next generation of precision medicines.