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SLAS Discov. 2019 Jan 7:2472555218816276. doi: 10.1177/2472555218816276. [Epub ahead of print]

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

Author information

1
1 EU-OPENSCREEN, Leibniz Research Institute for Molecular Pharmacology, Berlin, Germany.
2
2 Organic Synthesis Methodology Group, Latvian Institute of Organic Synthesis, Riga, Latvia.
3
3 Department of Biomedicine, University of Bergen, Bergen, Norway.
4
4 Centre for Molecular Medicine Norway-Nordic EMBL Partnership, University of Oslo, Oslo, Norway.
5
5 Fundación MEDINA, Health Sciences Technology Park, Granada, Spain.
6
6 Department of Experimental and Health Sciences, Universitat Pompeu Fabra, Barcelona, Catalunya, Spain.
7
7 IMIM Hospital del Mar Medical Research Institute, Research Program on Biomedical Informatics (GRIB), Barcelona, Spain.
8
8 Fraunhofer Institute for Molecular Biology and Applied Ecology IME, Screening Port, Hamburg, Germany.
9
9 Institute for Research in Molecular Medicine and Chronic Diseases-BioFarma Research Group, University of Santiago de Compostela, Santiago de Compostela, Spain.
10
10 Department of Molecular Probes and Prodrugs, Institute of Bioorganic Chemistry-Polish Academy of Sciences, Poznan, Poland.
11
11 Screening Platform, Principe Felipe Research Center, Valencia, Spain.
12
12 Drug Discovery Unit, Health Research Institute Hospital La Fe, Valencia, Spain.
13
13 Center for Nanomedicine and Theranostics, Department of Chemistry, Technical University of Denmark, Lyngby, Denmark.
14
14 Technical University of Denmark, DK-OPENSCREEN, Lyngby, Denmark.
15
15 Department of Bioinformatics, Institute of Biochemistry and Biophysics-Polish Academy of Sciences, Warsaw, Poland.
16
16 Department of Chemistry-CZ-OPENSCREEN, Masaryk University, Brno, Czech Republic.
17
17 The Arctic University of Norway, University of Tromsø, Marbio, Tromsø, Norway.
18
18 Screening Unit, Leibniz Research Institute for Molecular Pharmacology, Berlin, Germany.
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19 Medicinal Chemistry Research Group, Leibniz Research Institute for Molecular Pharmacology, Berlin, Germany.
20
20 Institute of Molecular Genetics of the ASCR, CZ-OPENSCREEN, Prague, Czech Republic.
21
21 Laboratory of Molecular Virology and Biological Chemistry, Institute of Medical Biology-Polish Academy of Sciences, Łódź, Poland.
22
22 Department of Immunology and Transfusion Medicine, Oslo University Hospital, Oslo, Norway.
23
23 Hybrid Technology Hub-Centre of Excellence-Institute of Basic Medical Sciences, University of Oslo, Oslo, Norway.
24
24 Faculty of Biochemistry and Molecular Medicine-Biocenter Oulu, University of Oulu, Oulu, Finland.
25
25 Working Group Compound Profiling and Screening, Helmholtz Centre for Infection Research, Brunswick, Germany.
26
26 Department of Chemical Biology, Helmholtz Centre for Infection Research, Brunswick, Germany.
27
27 German Center for Infection Research (DZIF), partner site Hannover-Brunswick, Brunswick, Germany.
28
28 Department of Cancer Immunology-Institute for Cancer Research, Oslo University Hospital, Oslo, Norway.
29
29 K.G. Jebsen Centre for Cancer Immunotherapy-Institute of Clinical Medicine, University of Oslo, Oslo, Norway.
30
30 K.G. Jebsen Centre for B Cell Malignancies-Institute of Clinical Medicine, University of Oslo, Oslo, Norway.
31
31 Institute of Diabetes and Regeneration Research, Helmholtz Centre Munich German Research Center for Environmental Health, Neuherberg, Germany.
32
32 Central Office, Berlin, EU-OPENSCREEN, Germany.

Abstract

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.

KEYWORDS:

chemical biology; compound library; medicinal chemistry; open access; screening

PMID:
30616481
DOI:
10.1177/2472555218816276

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