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New chemical warheads for covalent drug discovery

Project description

A closer look at covalent drug design

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.

Objective

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.

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Programme(s)

Topic(s)

Funding Scheme

HORIZON-ERC-POC - HORIZON ERC Proof of Concept Grants

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Call for proposal

(opens in new window) ERC-2024-POC

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Host institution

FUNDACIO INSTITUT CATALA D'INVESTIGACIO QUIMICA
Net EU contribution
€ 150 000,00
Address
AVENIDA PAISSOS CATALANS 16
43007 Tarragona
Spain
Region
Este Cataluña Tarragona
Activity type
Research Organisations
Links
Total cost
No data

Beneficiaries (1)