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EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology

P. Brennecke, D. Rasina, O. Aubi, K. Herzog, J. Landskron, B. Cautain, F. Vicente, J. Quintana, J. Mestres, B. Stechmann, B. Ellinger, J. Brea, JL. Kolanowski, R. Pilarski, M. Orzaez, A. Pineda-Lucena, L. Laraia, F. Nami, P. Zielenkiewicz, K....

. 2019 ; 24 (3) : 398-413. [pub] 20190107

Jazyk angličtina Země Spojené státy americké

Typ dokumentu časopisecké články, práce podpořená grantem

Perzistentní odkaz   https://www.medvik.cz/link/bmc20022881

Compound screening in biological assays and subsequent optimization of hits is indispensable for the development of new molecular research tools and drug candidates. To facilitate such discoveries, the European Research Infrastructure EU-OPENSCREEN was founded recently with the support of its member countries and the European Commission. Its distributed character harnesses complementary knowledge, expertise, and instrumentation in the discipline of chemical biology from 20 European partners, and its open working model ensures that academia and industry can readily access EU-OPENSCREEN's compound collection, equipment, and generated data. To demonstrate the power of this collaborative approach, this perspective article highlights recent projects from EU-OPENSCREEN partner institutions. These studies yielded (1) 2-aminoquinazolin-4(3 H)-ones as potential lead structures for new antimalarial drugs, (2) a novel lipodepsipeptide specifically inducing apoptosis in cells deficient for the pVHL tumor suppressor, (3) small-molecule-based ROCK inhibitors that induce definitive endoderm formation and can potentially be used for regenerative medicine, (4) potential pharmacological chaperones for inborn errors of metabolism and a familiar form of acute myeloid leukemia (AML), and (5) novel tankyrase inhibitors that entered a lead-to-candidate program. Collectively, these findings highlight the benefits of small-molecule screening, the plethora of assay designs, and the close connection between screening and medicinal chemistry within EU-OPENSCREEN.

Center for Nanomedicine and Theranostics Department of Chemistry Technical University of Denmark Lyngby Denmark 14 Technical University of Denmark DK OPENSCREEN Lyngby Denmark

Central Office Berlin EU OPENSCREEN Germany

Centre for Molecular Medicine Norway Nordic EMBL Partnership University of Oslo Oslo Norway

Centre for Molecular Medicine Norway Nordic EMBL Partnership University of Oslo Oslo Norway 28 Department of Cancer Immunology Institute for Cancer Research Oslo University Hospital Oslo Norway 29 K G Jebsen Centre for Cancer Immunotherapy Institute of Clinical Medicine University of Oslo Oslo Norway 30 K G Jebsen Centre for B Cell Malignancies Institute of Clinical Medicine University of Oslo Oslo Norway

Department of Bioinformatics Institute of Biochemistry and Biophysics Polish Academy of Sciences Warsaw Poland

Department of Biomedicine University of Bergen Bergen Norway

Department of Chemical Biology Helmholtz Centre for Infection Research Brunswick Germany 27 German Center for Infection Research partner site Hannover Brunswick Brunswick Germany

Department of Chemistry CZ OPENSCREEN Masaryk University Brno Czech Republic

Department of Experimental and Health Sciences Universitat Pompeu Fabra Barcelona Catalunya Spain

Department of Experimental and Health Sciences Universitat Pompeu Fabra Barcelona Catalunya Spain 7 IMIM Hospital del Mar Medical Research Institute Research Program on Biomedical Informatics Barcelona Spain

Department of Immunology and Transfusion Medicine Oslo University Hospital Oslo Norway 23 Hybrid Technology Hub Centre of Excellence Institute of Basic Medical Sciences University of Oslo Oslo Norway

Department of Molecular Probes and Prodrugs Institute of Bioorganic Chemistry Polish Academy of Sciences Poznan Poland

Drug Discovery Unit Health Research Institute Hospital La Fe Valencia Spain

EU OPENSCREEN Leibniz Research Institute for Molecular Pharmacology Berlin Germany

Faculty of Biochemistry and Molecular Medicine Biocenter Oulu University of Oulu Oulu Finland

Fraunhofer Institute for Molecular Biology and Applied Ecology IME Screening Port Hamburg Germany

Fundación MEDINA Health Sciences Technology Park Granada Spain

Institute for Research in Molecular Medicine and Chronic Diseases BioFarma Research Group University of Santiago de Compostela Santiago de Compostela Spain

Institute of Diabetes and Regeneration Research Helmholtz Centre Munich German Research Center for Environmental Health Neuherberg Germany

Institute of Molecular Genetics of the ASCR CZ OPENSCREEN Prague Czech Republic

Laboratory of Molecular Virology and Biological Chemistry Institute of Medical Biology Polish Academy of Sciences Łódź Poland

Medicinal Chemistry Research Group Leibniz Research Institute for Molecular Pharmacology Berlin Germany

Organic Synthesis Methodology Group Latvian Institute of Organic Synthesis Riga Latvia

Screening Platform Principe Felipe Research Center Valencia Spain

Screening Unit Leibniz Research Institute for Molecular Pharmacology Berlin Germany

The Arctic University of Norway University of Tromsø Marbio Tromsø Norway

Working Group Compound Profiling and Screening Helmholtz Centre for Infection Research Brunswick Germany

Citace poskytuje Crossref.org

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