Project description
Large-scale drug discovery
There is a pressing need for new drugs that selectively target and inhibit human proteins such as solute carriers and E3-ubiquitin ligases. The EU-funded EUbOPEN project aims to generate the largest freely available library of compounds covering one third of the druggable genome. Partners will characterise the selectivity, potency and cellular activity of protein inhibitors with particular focus on inflammatory bowel disease, cancer and neurodegeneration. The generated technologies are expected to significantly shorten hit to lead identification processes and advance the overall drug discovery pipeline. EUbOPEN will partner with other large projects to coordinate drug discovery efforts at a global level.
Objective
The EUbOPEN partnership of excellence will aim to generate the largest freely available set of high-quality chemical inhibitors for human proteins. These compounds will include chemical probes for solute carriers (SLCs), E3-ubiquitin ligases (E3s) and other proteins, and a chemogenomic library (CGL) of 3000-5000 compounds covering one third of the druggable genome. All compounds in the sets will be comprehensively characterised defining their selectivity, potency and cellular activity. The compounds will be annotated with a series of established and novel biochemical and cell-based assays, including many derived from primary patient cells. Diseases of particular focus will be inflammatory bowel disease, cancer and neurodegeneration.
EUbOPEN partners have proven track records leading large international open science projects, developing unencumbered key reagents, and exploring new target areas. A strong commitment to open data and open science will accelerate the dissemination of knowledge and reagents as well as mitigate ethical issues that might arise by working with patient-derived cells.
EUbOPEN will partner extensively with other large projects (e.g. ReSOLUTE, Illuminating the Druggable Genome) to minimize duplication of effort and to maximize global coordination. EUbOPEN will provide via the EFPIA partners the public access to industry’s deep medicinal chemistry skills.
Sustainability of the project’s resources will be ensured through already established partnerships with chemical vendors and cheminformatics/database providers, which will ensure the long-term availability of the new chemical tool sets, all associated profiling data and established protocols.
The EUbOPEN project will form the foundation for future efforts to generate chemical modulators for the entire druggable genome and will develop new technologies significantly shortening hit and lead identification processes.
Fields of science
- medical and health sciencesbasic medicinemedicinal chemistry
- medical and health sciencesclinical medicinegastroenterologyinflammatory bowel disease
- natural sciencesbiological sciencesbiochemistrybiomoleculesproteins
- medical and health sciencesclinical medicineoncology
- natural sciencesbiological sciencesgeneticsgenomes
Keywords
Programme(s)
Topic(s)
Funding Scheme
RIA - Research and Innovation actionCoordinator
60323 Frankfurt Am Main
Germany
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Participants (22)
OX1 2JD Oxford
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17177 Stockholm
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2333 ZA Leiden
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8092 Zuerich
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60596 Frankfurt
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69117 Heidelberg
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DD1 4HN Dundee
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80686 Munchen
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NW1 2BE London
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27599 Chapel Hill
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M5S 1A1 Toronto
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51373 Leverkusen
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55218 Ingelheim
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CT13 9NJ Sandwich
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8152 Glattpark
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91190 GIF-SUR-YVETTE
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100 44 Stockholm
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0X11 0DE Didcot
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M5G 0 A3 TORONTO, ONTARIO
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H3A0G4 Montreal
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Participation ended
CAMBRIDGE MA
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80539 MUNCHEN
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