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

Autor:	Gabriele Bassi, Nicholas Favalli, Miriam Vuk, Marco Catalano, Adriano Martinelli, Anika Trenner, Antonio Porro, Su Yang, Chuin Lean Tham, Mustafa Moroglu, Wyatt W. Yue, Stuart J. Conway, Peter K. Vogt, Alessandro A. Sartori, Jörg Scheuermann, Dario Neri
Jazyk:	angličtina
Rok vydání:	2020
Předmět:	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) Science
Zdroj:	Advanced Science, Vol 7, Iss 22, Pp n/a-n/a (2020)
Druh dokumentu:	article
ISSN:	2198-3844
DOI:	10.1002/advs.202001970
Popis:	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.
Databáze:	Directory of Open Access Journals
Externí odkaz:	https://doaj.org/article/6523af672d2b411ba7e7080f84e45492 Zobrazit plný text záznamu View record in DOAJ Plný text ve formátu PDF Plný text ve formátu HTML
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