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

J 2019

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

BRENNECKE, Philip; Dace RASINA; Oscar AUBI; Katja HERZOG; Johannes LANDSKRON et al.

Základní údaje

Originální název

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

Autoři

BRENNECKE, Philip; Dace RASINA; Oscar AUBI; Katja HERZOG; Johannes LANDSKRON; Bastien CAUTAIN; Francisca VICENTE; Jordi QUINTANA; Jordi MESTRES; Bahne STECHMANN; Bernhard ELLINGER; Jose BREA; Jacek L. KOLANOWSKI; Radosław PILARSKI; Mar ORZAEZ; Antonio PINEDA-LUCENA; Luca LARAIA; Faranak NAMI; Piotr ZIELENKIEWICZ; Kamil PARUCH; Espen HANSEN; Jens P. VON KRIES; Martin NEUENSCHWANDER; Edgar SPECKER; Petr BARTŮNĚK; Šárka SIMOVA; Zbigniew LESNIKOWSKI; Stefan KRAUSS; Lari LEHTIO; Ursula BILITEWSKI; Mark BRONSTRUP; Kjetil TASKEN; Aigars JIRGENSONS; Heiko LICKERT; Mads H. CLAUSEN; Jeanette H. ANDERSEN; Maria J. VICENT; Olga GENILLOUD; Aurora MARTINEZ; Marc NAZARE; Wolfgang FECKE a Philip GRIBBON

Vydání

SLAS DISCOVERY, THOUSAND OAKS, SAGE PUBLICATIONS INC, 2019, 2472-5552

Další údaje

Jazyk

angličtina

Typ výsledku

Článek v odborném periodiku

Obor

10401 Organic chemistry

Stát vydavatele

Spojené státy

Utajení

není předmětem státního či obchodního tajemství

Odkazy

Full Text

Impakt faktor

Impact factor: 2.195

Označené pro přenos do RIV

Ano

Kód RIV

RIV/00216224:14310/19:00109267

Organizační jednotka

Přírodovědecká fakulta

Klíčová slova anglicky

chemical biology; screening; medicinal chemistry; open access; compound library

Štítky

rivok

Příznaky

Mezinárodní význam, Recenzováno

Změněno: 11. 5. 2020 13:20, Mgr. Marie Novosadová Šípková, DiS.

Anotace

V originále

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.

Návaznosti

LM2015063, projekt VaV

Název: Národní infrastruktura chemické biologie (Akronym: CZ-OPENSCREEN)

Investor: Ministerstvo školství, mládeže a tělovýchovy ČR, CZ-OPENSCREEN: National Infrastructure for Chemical Biology

Citovat

@article{1505081,
   author = {Brennecke, Philip and Rasina, Dace and Aubi, Oscar and Herzog, Katja and Landskron, Johannes and Cautain, Bastien and Vicente, Francisca and Quintana, Jordi and Mestres, Jordi and Stechmann, Bahne and Ellinger, Bernhard and Brea, Jose and Kolanowski, Jacek L. and Pilarski, Radosław and Orzaez, Mar and PinedaandLucena, Antonio and Laraia, Luca and Nami, Faranak and Zielenkiewicz, Piotr and Paruch, Kamil and Hansen, Espen and von Kries, Jens P. and Neuenschwander, Martin and Specker, Edgar and Bartůněk, Petr and Simova, Šárka and Lesnikowski, Zbigniew and Krauss, Stefan and Lehtio, Lari and Bilitewski, Ursula and Bronstrup, Mark and Tasken, Kjetil and Jirgensons, Aigars and Lickert, Heiko and Clausen, Mads H. and Andersen, Jeanette H. and Vicent, Maria J. and Genilloud, Olga and Martinez, Aurora and Nazare, Marc and Fecke, Wolfgang and Gribbon, Philip},
   article_location = {THOUSAND OAKS},
   article_number = {3},
   doi = {https://doi.org/10.1177/2472555218816276},
   keywords = {chemical biology; screening; medicinal chemistry; open access; compound library},
   language = {eng},
   issn = {2472-5552},
   journal = {SLAS DISCOVERY},
   title = {EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology},
   url = {https://journals.sagepub.com/doi/10.1177/2472555218816276},
   volume = {24},
   year = {2019}
}

TY  - JOUR
ID  - 1505081
AU  - Brennecke, Philip - Rasina, Dace - Aubi, Oscar - Herzog, Katja - Landskron, Johannes - Cautain, Bastien - Vicente, Francisca - Quintana, Jordi - Mestres, Jordi - Stechmann, Bahne - Ellinger, Bernhard - Brea, Jose - Kolanowski, Jacek L. - Pilarski, Radosław - Orzaez, Mar - Pineda-Lucena, Antonio - Laraia, Luca - Nami, Faranak - Zielenkiewicz, Piotr - Paruch, Kamil - Hansen, Espen - von Kries, Jens P. - Neuenschwander, Martin - Specker, Edgar - Bartůněk, Petr - Simova, Šárka - Lesnikowski, Zbigniew - Krauss, Stefan - Lehtio, Lari - Bilitewski, Ursula - Bronstrup, Mark - Tasken, Kjetil - Jirgensons, Aigars - Lickert, Heiko - Clausen, Mads H. - Andersen, Jeanette H. - Vicent, Maria J. - Genilloud, Olga - Martinez, Aurora - Nazare, Marc - Fecke, Wolfgang - Gribbon, Philip
PY  - 2019
TI  - EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology
JF  - SLAS DISCOVERY
VL  - 24
IS  - 3
SP  - 398-413
EP  - 398-413
PB  - SAGE PUBLICATIONS INC
SN  - 24725552
KW  - chemical biology
KW  - screening
KW  - medicinal chemistry
KW  - open access
KW  - compound library
UR  - https://journals.sagepub.com/doi/10.1177/2472555218816276
L2  - https://journals.sagepub.com/doi/10.1177/2472555218816276
N2  - 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.
ER  -

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