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

0506196 - ÚMG 2020 RIV US eng J - Journal Article
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. - Bartůněk, Petr - Šímová, Šárka - Lesnikowski, Z. - Krauss, S. - Lehtio, L. - Bilitewski, U. - Broenstrup, M. - Tasken, K. - Jirgensons, A. - Lickert, H. - Clausen, M. H. - Andersen, J. H. - Vicent, M. J. - Genilloud, O. - Martinez, A. - Nazare, M. - Fecke, W. - Gribbon, P.
EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology.
SLAS Discovery. Roč. 24, č. 3 (2019), s. 398-413. ISSN 2472-5552. E-ISSN 2472-5560
R&D Projects: GA MŠMT LO1220; GA MŠMT LM2015063
Institutional support: RVO:68378050
Keywords : chemical biology * screening * medicinal chemistry * open access * compound library
OECD category: Biochemical research methods
Impact factor: 2.195, year: 2019
Method of publishing: Open access
https://journals.sagepub.com/doi/10.1177/2472555218816276

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.
Permanent Link: http://hdl.handle.net/11104/0297510