A Single‐Stranded DNA‐Encoded Chemical Library Based on a Stereoisomeric Scaffold Enables Ligand Discovery by Modular Assembly of Building Blocks
dc.contributor.author
Bassi, Gabriele
dc.contributor.author
Favalli, Nicholas
dc.contributor.author
Vuk, Miriam
dc.contributor.author
Catalano, Marco
dc.contributor.author
Martinelli, Adriano
dc.contributor.author
Trenner, Anika
dc.contributor.author
Porro, Antonio
dc.contributor.author
Yang, Su
dc.contributor.author
Tham, Chuin Lean
dc.contributor.author
Moroglu, Mustafa
dc.contributor.author
Yue, Wyatt W.
dc.contributor.author
Conway, Stuart J.
dc.contributor.author
Vogt, Peter K.
dc.contributor.author
Sartori, Alessandro A.
dc.contributor.author
Scheuermann, Jörg
dc.contributor.author
Neri, Dario
dc.date.accessioned
2020-11-27T06:53:44Z
dc.date.available
2020-11-01T08:20:20Z
dc.date.available
2020-11-02T12:54:00Z
dc.date.available
2020-11-27T06:53:44Z
dc.date.issued
2020-11-18
dc.identifier.issn
2198-3844
dc.identifier.other
10.1002/advs.202001970
en_US
dc.identifier.uri
http://hdl.handle.net/20.500.11850/448986
dc.identifier.doi
10.3929/ethz-b-000448986
dc.description.abstract
A versatile and Lipinski‐compliant DNA‐encoded library (DEL), comprising 366 600 glutamic acid derivatives coupled to oligonucleotides serving as amplifiable identification barcodes is designed, constructed, and characterized. The GB‐DEL library, constructed in single‐stranded DNA format, allows de novo identification of specific binders against several pharmaceutically relevant proteins. Moreover, hybridization of the single‐stranded DEL with a set of known protein ligands of low to medium affinity coupled to a complementary DNA strand results in self‐assembled selectable chemical structures, leading to the identification of affinity‐matured compounds.
en_US
dc.format
application/pdf
en_US
dc.language.iso
en
en_US
dc.publisher
Wiley
en_US
dc.rights.uri
http://creativecommons.org/licenses/by/4.0/
dc.subject
Human alpha-aminoadipic semialdehyde synthase (AASS)
en_US
dc.subject
Affinity maturation
en_US
dc.subject
Cyclic-AMP response element binding protein (CREBBP)
en_US
dc.subject
DNA-encoded chemical libraries (DEL)
en_US
dc.subject
Drug discovery
en_US
dc.subject
Encoded self-assembling chemical libraries (ESAC)
en_US
dc.subject
FANCD2-associated nuclease 1 (FAN-1)
en_US
dc.subject
Phosphatidylinositol 3-kinase (PI3K)
en_US
dc.title
A Single‐Stranded DNA‐Encoded Chemical Library Based on a Stereoisomeric Scaffold Enables Ligand Discovery by Modular Assembly of Building Blocks
en_US
dc.type
Journal Article
dc.rights.license
Creative Commons Attribution 4.0 International
dc.date.published
2020-10-14
ethz.journal.title
Advanced Science
ethz.journal.volume
7
en_US
ethz.journal.issue
22
en_US
ethz.journal.abbreviated
Adv. Sci.
ethz.pages.start
2001970
en_US
ethz.size
10 p.
en_US
ethz.version.deposit
publishedVersion
en_US
ethz.grant
Understanding and Exploiting the Molecular Targeting of Tumor Neo-vasculature
en_US
ethz.grant
Fulfilling Paul Ehrlich’s Dream: therapeutics with activation on demand
en_US
ethz.grant
Unrestricted Leveraging of Targets for Research Advancement and Drug Discovery
en_US
ethz.identifier.wos
ethz.identifier.scopus
ethz.publication.place
Weinheim
en_US
ethz.publication.status
published
en_US
ethz.leitzahl
ETH Zürich::00002 - ETH Zürich::00012 - Lehre und Forschung::00007 - Departemente::02020 - Dep. Chemie und Angewandte Biowiss. / Dep. of Chemistry and Applied Biosc.::02534 - Institut für Pharmazeutische Wiss. / Institute of Pharmaceutical Sciences::03463 - Neri, Dario (ehemalig) / Neri, Dario (former)
ethz.leitzahl
ETH Zürich::00002 - ETH Zürich::00012 - Lehre und Forschung::00007 - Departemente::02020 - Dep. Chemie und Angewandte Biowiss. / Dep. of Chemistry and Applied Biosc.::02534 - Institut für Pharmazeutische Wiss. / Institute of Pharmaceutical Sciences::08641 - DNA-encoded Chemical Libraries / DNA-encoded Chemical Libraries
ethz.leitzahl.certified
ETH Zürich::00002 - ETH Zürich::00012 - Lehre und Forschung::00007 - Departemente::02020 - Dep. Chemie und Angewandte Biowiss. / Dep. of Chemistry and Applied Biosc.::02534 - Institut für Pharmazeutische Wiss. / Institute of Pharmaceutical Sciences::03463 - Neri, Dario (ehemalig) / Neri, Dario (former)
ethz.grant.agreementno
182003
ethz.grant.agreementno
670603
ethz.grant.agreementno
115766
ethz.grant.fundername
SNF
ethz.grant.fundername
EC
ethz.grant.fundername
EC
ethz.grant.funderDoi
10.13039/501100001711
ethz.grant.funderDoi
10.13039/501100000780
ethz.grant.funderDoi
10.13039/501100000780
ethz.grant.program
H2020
ethz.grant.program
FP7
ethz.grant.program
Projekte Lebenswissenschaften
ethz.date.deposited
2020-11-01T08:20:28Z
ethz.source
WOS
ethz.eth
yes
en_US
ethz.availability
Open access
en_US
ethz.rosetta.installDate
2020-11-27T06:53:56Z
ethz.rosetta.lastUpdated
2022-03-29T04:06:47Z
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true
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