A Single‐Stranded DNA‐Encoded Chemical Library Based on a Stereoisomeric Scaffold Enables Ligand Discovery by Modular Assembly of Building Blocks
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Date
2020-11-18
Publication Type
Journal Article
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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.
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published
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Journal / series
Volume
7 (22)
Pages / Article No.
2001970
Publisher
Wiley
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Software
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Subject
Human alpha-aminoadipic semialdehyde synthase (AASS); Affinity maturation; Cyclic-AMP response element binding protein (CREBBP); DNA-encoded chemical libraries (DEL); Drug discovery; Encoded self-assembling chemical libraries (ESAC); FANCD2-associated nuclease 1 (FAN-1); Phosphatidylinositol 3-kinase (PI3K)
Organisational unit
03463 - Neri, Dario (ehemalig) / Neri, Dario (former)
08641 - Scheuermann, Jörg (Tit.-Prof.) / Scheuermann, Jörg (Tit.-Prof.)
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Funding
182003 - Understanding and Exploiting the Molecular Targeting of Tumor Neo-vasculature (SNF)
670603 - Fulfilling Paul Ehrlich’s Dream: therapeutics with activation on demand (EC)
115766 - Unrestricted Leveraging of Targets for Research Advancement and Drug Discovery (EC)
670603 - Fulfilling Paul Ehrlich’s Dream: therapeutics with activation on demand (EC)
115766 - Unrestricted Leveraging of Targets for Research Advancement and Drug Discovery (EC)