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 Floriani, José Manuel
A1 Kolanowski, Jacek L.
A1 Pilarsk, Radosław
A1 Orzaez, Mar
A1 Pineda-Lucena, Antonio
A1 Laraia, Luca
A1 Nam, Faranak
A1 Zielenkiewicz, Piotr
A1 Paruch, Kamil
A1 Hansen, Espen
A1 Kries, Jens P. von
A1 Neuenschwander, Martin
A1 Specker, Edgar
A1 Bartunek, Petr
A1 Simova, Sarka
A1 Lesnikowski, 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 Martínez, Aurora
A1 Nazaré, Marc
A1 Fecke, Wolfgang
A1 Gribbon, Philip
K1 Chemical biology
K1 Screening
K1 Medicinal chemistry
K1 Open access
K1 Compound library
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(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.
PB SAGE Publications
SN 2472-5552
YR 2019
FD 2019
LK http://hdl.handle.net/10347/21237
UL http://hdl.handle.net/10347/21237
LA eng
NO 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 the Science of Drug Discovery, 24(3), 398–413. https://doi.org/10.1177/2472555218816276
NO The  authors  disclosed  receipt  of  the  following  financial  support  for  the  research,  authorship,  and/or  publication  of  this  article:  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.). 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   the   European   Regional Development Fund (agreement no. 1.1.1.1/16/A/290) for financial  support.  L.L.  acknowledges  the  Academy  of  Finland  (grant  nos.  287063  and  294085)  and  the  Jane  and  Aatos  Erkko  Foundation  for  funding.  EU-OPENSCREEN  acknowledges  its  member and observer states for funding and support. P. Bartunek acknowledges  MEYS  (LO1220  and  LM2015063)  for  funding.  P.G.  and  H.L.  acknowledge  funding  from  the  German  Federal  Ministry of Education and Research. J.L.K. and R.P. acknowledge financial support from the Polish Ministry of Science and Higher Education  (KNOW  program  and  POL-OPENSCREEN  project  number  401086).  M.J.V.  acknowledges  the  European  Regional  Development  Fund  and  the  Conselleria  de  Sanitat  Universal  i  Salut Pública (Generalitat Valenciana, GVA)
DS Minerva
RD 24 abr 2026