University of Oulu

Brennecke, P., Rasina, D., Aubi, O., Herzog, K., Landskron, J., Cautain, B., … Gribbon, P. (2019). EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology. SLAS DISCOVERY: Advancing Life Sciences R&D, 24(3), 398–413.

EU-OPENSCREEN : a novel collaborative approach to facilitate chemical biology

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Author: Brennecke, Philip1; Rasina, Dace2; Aubi, Oscar3;
Organizations: 1EU-OPENSCREEN, Leibniz Research Institute for Molecular Pharmacology, Berlin, Germany
2Organic Synthesis Methodology Group, Latvian Institute of Organic Synthesis, Riga, Latvia
3Department of Biomedicine, University of Bergen, Bergen, Norway
4Centre for Molecular Medicine Norway–Nordic EMBL Partnership, University of Oslo, Oslo, Norway
5Fundación MEDINA, Health Sciences Technology Park, Granada, Spain
6Department of Experimental and Health Sciences, Universitat Pompeu Fabra, Barcelona, Catalunya, Spain
7IMIM Hospital del Mar Medical Research Institute, Research Program on Biomedical Informatics (GRIB), Barcelona, Spain
8Fraunhofer Institute for Molecular Biology and Applied Ecology IME, Screening Port, Hamburg, Germany
9Institute for Research in Molecular Medicine and Chronic Diseases—BioFarma Research Group, University of Santiago de Compostela, Santiago de Compostela, Spain
10Department of Molecular Probes and Prodrugs, Institute of Bioorganic Chemistry—Polish Academy of Sciences, Poznan, Poland
11Screening Platform, Principe Felipe Research Center, Valencia, Spain
12Drug Discovery Unit, Health Research Institute Hospital La Fe, Valencia, Spain
13Center for Nanomedicine and Theranostics, Department of Chemistry, Technical University of Denmark, Lyngby, Denmark
14Technical University of Denmark, DK-OPENSCREEN, Lyngby, Denmark
15Department of Bioinformatics, Institute of Biochemistry and Biophysics—Polish Academy of Sciences, Warsaw, Poland
16Department of Chemistry—CZ-OPENSCREEN, Masaryk University, Brno, Czech Republic
17The Arctic University of Norway, University of Tromsø, Marbio, Tromsø, Norway
18Screening Unit, Leibniz Research Institute for Molecular Pharmacology, Berlin, Germany
19Medicinal Chemistry Research Group, Leibniz Research Institute for Molecular Pharmacology, Berlin, Germany
20Institute of Molecular Genetics of the ASCR, CZ-OPENSCREEN, Prague, Czech Republic
21Laboratory of Molecular Virology and Biological Chemistry, Institute of Medical Biology—Polish Academy of Sciences, Łódź, Poland
22Department of Immunology and Transfusion Medicine, Oslo University Hospital, Oslo, Norway
23Hybrid Technology Hub -Centre of Excellence - Institute of Basic Medical Sciences, University of Oslo, Oslo, Norway
24Faculty of Biochemistry and Molecular Medicine—Biocenter Oulu, University of Oulu, Oulu, Finland
25Working Group Compound Profiling and Screening, Helmholtz Centre for Infection Research, Brunswick, Germany
26Department of Chemical Biology, Helmholtz Centre for Infection Research, Brunswick, Germany
27German Center for Infection Research (DZIF), partner site Hannover-Brunswick, Brunswick, Germany
28Department of Cancer Immunology—Institute for Cancer Research, Oslo University Hospital, Oslo, Norway
29K.G. Jebsen Centre for Cancer Immunotherapy—Institute of Clinical Medicine, University of Oslo, Oslo, Norway
30K.G. Jebsen Centre for B Cell Malignancies—Institute of Clinical Medicine, University of Oslo, Oslo, Norway
31Institute of Diabetes and Regeneration Research, Helmholtz Centre Munich German Research Center for Environmental Health, Neuherberg, Germany
32Central Office, Berlin, EU-OPENSCREEN, Germany
Format: article
Version: accepted version
Access: open
Online Access: PDF Full Text (PDF, 10.3 MB)
Persistent link:
Language: English
Published: SAGE Publications, 2019
Publish Date: 2019-08-14


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(3H)-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.

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Series: SLAS discovery
ISSN: 2472-5552
ISSN-E: 2472-5560
ISSN-L: 2472-5552
Volume: 24
Issue: 3; SI
Pages: 398 - 413
DOI: 10.1177/2472555218816276
Type of Publication: A1 Journal article – refereed
Field of Science: 1182 Biochemistry, cell and molecular biology
Funding: NOR-OPENSCREEN, funded by the Research Council of Norway (RCN), and the K.G. Jebsen Centre for Neuropsychiatric disorders, for financial support (to A.M.). Jarl Underhaug is acknowledged for developing the in-house software for DSF screening. The Danish Research Infrastructure for Chemical Biology, DK-OPENSCREEN, acknowledges financial support from the Ministry of Higher Education and Science (grant case no. 5072-00019B), the Technical University of Denmark and the other contributing universities.The Latvian Institute of Organic Synthesis acknowledges European Regional Development Fund (Agreement No. for financial support. L.L. acknowledges the Academy of Finland (grant no. 287063 and 294085) and the Jane and Aatos Erkko foundation for funding.EU-OPENSCREEN acknowledges its member and observer states for funding and support. Petr Bartunek acknowledges MEYS (LO1220, LM2015063) for funding.
Academy of Finland Grant Number: 287063
Detailed Information: 287063 (Academy of Finland Funding decision)
294085 (Academy of Finland Funding decision)
Copyright information: © 2019 American Chemical Society. Published in this repository with the kind permission of the publisher.