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Brennecke, P.* ; Rasina, D.* ; Aubi, O.* ; Herzog, K.* ; Landskron, J.* ; Cautain, B.* ; Vicente, F.* ; Quintana, J.* ; Mestres, J.* ; Stechmann, B.* ; Ellinger, B.* ; Brea, J.* ; Kolanowski, J.L.* ; Pilarski, R.* ; Orzaez, M.* ; Pineda-Lucena, A.* ; Laraia, L.* ; Nami, F.* ; Zielenkiewicz, P.* ; Paruch, K.* ; Hansen, E.* ; von Kries, J.P.* ; Neuenschwander, M.* ; Specker, E.* ; Bartunek, P.* ; Simova, S.* ; Leśnikowski, Z.* ; Krauss, S.* ; Lehtiö, L.* ; Bilitewski, U.* ; Brönstrup, M.* ; Taskén, K.* ; Jirgensons, A.* ; Lickert, H. ; Clausen, M.H.* ; Andersen, J.H.* ; Vicent, M.J.* ; Genilloud, O.* ; Martinez, A.* ; Nazaré, M.* ; Fecke, W.* ; Gribbon, P.*

EU-OPENSCREEN: A novel collaborative approach to facilitate chemical biology.

SLAS Discov. 24, 398-413 (2019)
Verlagsversion Forschungsdaten DOI PMC
Open Access Hybrid
Creative Commons Lizenzvertrag
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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2.192
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6
6
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Publikationstyp Artikel: Journalartikel
Dokumenttyp Review
Schlagwörter Chemical Biology ; Screening ; Medicinal Chemistry ; Open Access ; Compound Library; Renal-cell Carcinoma; Von-hippel-lindau; Drug Discovery; Structural Basis; Pharmacological Chaperones; Potent Inhibitors; Screening Assay; Plasmepsins I; Beta-cells; Molecule
Sprache englisch
Veröffentlichungsjahr 2019
HGF-Berichtsjahr 2019
ISSN (print) / ISBN 2472-5552
e-ISSN 2472-5560
Zeitschrift SLAS Discovery
Quellenangaben Band: 24, Heft: 3, Seiten: 398-413 Artikelnummer: , Supplement: ,
Verlag Sage
Verlagsort Thousand Oaks, Calif.
Begutachtungsstatus Peer reviewed
Institut(e) Institute of Diabetes and Regeneration Research (IDR)
POF Topic(s) 30201 - Metabolic Health
Forschungsfeld(er) Helmholtz Diabetes Center
PSP-Element(e) G-502300-001
DOI 10.1177/2472555218816276
WOS ID WOS:000459287100016
Scopus ID 85060055493
PubMed ID 30616481
Erfassungsdatum 2019-03-04
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