Objectif In this STREP we intend to use cutting-edge nuclear magnetic resonance (NMR) techniques to develop a fast, integrated approach to support structure-based drug design. The project will speed up drug design efforts for typical drug targets and will shorten t he lead-time for new drugs. We will develop fast, reliable and robust NMR techniques for exact structural and dynamic characterization of drug-receptor interactions at atomic resolution, thus enabling and/or improving the potential for directed development of drugs exhibiting a maximum of desired interaction characteristics in a relatively short time. Protocols for obtaining the NMR data needed for the characterization of proteins, inhibitors and protein-inhibitor complexes will be developed, starting from known X-ray structures, thus establishing a tight connection between NMR and X-ray technology and exploiting optimally the complementary strengths of both techniques. The new NMR technologies will be complemented by computer modelling for protein-inhibito r complexes and by advanced tailored protein expression methods. In order to show the impact for drug development, the new approach will aim at phosphatases, a major class of drug targets with broad medical implications. A majority of cellular functions d epend on phosphorylation by kinases and de-phosphorylation by phosphatases. High eukaryotes encode approximately 500 kinase and 100 phosphatase schemes, corresponding to 3% of the genome. While the importance of kinases in cellular regulation led to substa ntial drug design activities, the importance of phosphatases has only been appreciated recently. Phosphatases regulate insulin signalling, cell growth and the cell cycle. Therefore, the inhibition of phosphatases is perused for the treatment of diabetes, o besity and various cancers. Human genome data provide access to a broad range of phosphatases, allowing systematic drug design using advanced techniques to identify potential inhibitors. Champ scientifique medical and health sciencesbasic medicinepharmacology and pharmacydrug discoverymedical and health sciencesbasic medicinemedicinal chemistrynatural sciencesbiological sciencesbiochemistrybiomoleculesproteinsmedical and health sciencesclinical medicineendocrinologydiabetesmedical and health sciencesclinical medicinepneumologytuberculosis Mots‑clés Drug design NMR Spectroscopy Phosphatases Structural genomics Programme(s) FP6-LIFESCIHEALTH - Life sciences, genomics and biotechnology for health: Thematic Priority 1 under the Focusing and Integrating Community Research programme 2002-2006. Thème(s) LSH-2003-1.1.0-1 - Topics for Specific Targeted Research Project in the area of Fundamental knowledge and basic tools for functional genomics in all organisms Appel à propositions FP6-2003-LIFESCIHEALTH-I Voir d’autres projets de cet appel Régime de financement STIP - Specific Targeted Innovation Project Coordinateur UTRECHT UNIVERSITY, FACULTY OF CHEMISTRY, BIJVOET CENTER FOR BIOMOLECULAR RESEARCH, Contribution de l’UE Aucune donnée Adresse Heidelberglaan 8 UTRECHT Pays-Bas Voir sur la carte Liens Site web Opens in new window Coût total Aucune donnée Participants (5) Trier par ordre alphabétique Trier par contribution de l’UE Tout développer Tout réduire JOHANN WOLFGANG GOETHE-UNIVERSITY Allemagne Contribution de l’UE Aucune donnée Adresse Senckenberganlage 31 FRANKFURT/ MAIN Voir sur la carte Liens Site web Opens in new window Coût total Aucune donnée CONSORZIO INTERUNIVERSITARIO RISONANZE MAGNETICHE DI METALLPROTEINE PARAMAGNETICHE Italie Contribution de l’UE Aucune donnée Adresse Via Luigi Sacconi, 6 SESTO FIORENTINO Voir sur la carte Liens Site web Opens in new window Coût total Aucune donnée THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL Royaume-Uni Contribution de l’UE Aucune donnée Adresse 123 Old Brompton Road LONDON Voir sur la carte Liens Site web Opens in new window Coût total Aucune donnée SYNTHACON GMBH Allemagne Contribution de l’UE Aucune donnée Adresse Am Haupttor - Gebäude 4310 LEUNA Voir sur la carte Liens Site web Opens in new window Coût total Aucune donnée MEDIZINISCHE UNIVERSITÄT WIEN (MEDICAL UNIVERSITY VIENNA) Autriche Contribution de l’UE Aucune donnée Adresse Spitalgasse 23 VIENNA Voir sur la carte Liens Site web Opens in new window Coût total Aucune donnée