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A Single-Stranded DNA-Encoded Chemical Library Based on a Stereoisomeric Scaffold Enables Ligand Discovery by Modular Assembly of Building Blocks


Bassi, Gabriele; Favalli, Nicholas; Vuk, Miriam; Catalano, Marco; Martinelli, Adriano; Trenner, Anika; Porro, Antonio; Yang, Su; Tham, Chuin Lean; Moroglu, Mustafa; Yue, Wyatt W; Conway, Stuart J; Vogt, Peter K; Sartori, Alessandro A; Scheuermann, Jörg; Neri, Dario (2020). A Single-Stranded DNA-Encoded Chemical Library Based on a Stereoisomeric Scaffold Enables Ligand Discovery by Modular Assembly of Building Blocks. Advanced Science, 7(22):2001970.

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.

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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Item Type:Journal Article, refereed, original work
Communities & Collections:04 Faculty of Medicine > Institute of Molecular Cancer Research
07 Faculty of Science > Institute of Molecular Cancer Research
Dewey Decimal Classification:570 Life sciences; biology
610 Medicine & health
Scopus Subject Areas:Health Sciences > Medicine (miscellaneous)
Physical Sciences > General Chemical Engineering
Life Sciences > Biochemistry, Genetics and Molecular Biology (miscellaneous)
Physical Sciences > General Materials Science
Physical Sciences > General Engineering
Physical Sciences > General Physics and Astronomy
Language:English
Date:November 2020
Deposited On:09 Feb 2021 13:04
Last Modified:10 Feb 2021 21:00
Publisher:Wiley Open Access
ISSN:2198-3844
OA Status:Gold
Free access at:Publisher DOI. An embargo period may apply.
Publisher DOI:https://doi.org/10.1002/advs.202001970
PubMed ID:33240760

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