RT Journal Article
T1 EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology.
A1 Brennecke, Philip
A1 Rasina, Dace
A1 Aubi, Oscar
A1 Herzog, Katja
A1 Landskron, Johannes
A1 Cautain, Bastien
A1 Vicente, Francisca
A1 Quintana, Jordi
A1 Mestres, Jordi
A1 Stechmann, Bahne
A1 Ellinger, Bernhard
A1 Brea, Jose
A1 Kolanowski, Jacek L
A1 Pilarski, Radosław
A1 Orzaez, Mar
A1 Pineda-Lucena, Antonio
A1 Laraia, Luca
A1 Nami, Faranak
A1 Zielenkiewicz, Piotr
A1 Paruch, Kamil
A1 Hansen, Espen
A1 von Kries, Jens P
A1 Neuenschwander, Martin
A1 Specker, Edgar
A1 Bartunek, Petr
A1 Simova, Sarka
A1 Leśnikowski, Zbigniew
A1 Krauss, Stefan
A1 Lehtiö, Lari
A1 Bilitewski, Ursula
A1 Brönstrup, Mark
A1 Taskén, Kjetil
A1 Jirgensons, Aigars
A1 Lickert, Heiko
A1 Clausen, Mads H
A1 Andersen, Jeanette H
A1 Vicent, Maria J
A1 Genilloud, Olga
A1 Martinez, Aurora
A1 Nazaré, Marc
A1 Fecke, Wolfgang
A1 Gribbon, Philip
K1 chemical biology
K1 compound library
K1 medicinal chemistry
K1 open access
K1 screening
AB 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.
YR 2019
FD 2019-01-07
LK http://hdl.handle.net/10668/13382
UL http://hdl.handle.net/10668/13382
LA en
DS RISalud
RD Apr 8, 2025