Journal
ADVANCED SCIENCE
Volume 7, Issue 22, Pages -Publisher
WILEY
DOI: 10.1002/advs.202001970
Keywords
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)
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Funding
- ETH Zurich
- Swiss National Science Foundation [31003A_176161, 310030_182003/1]
- European Research Council (ERC) under the European Union [670603]
- National Cancer Institute [R35 CA197582]
- EPSRC Centre for Doctoral Training in Synthesis for Biology and Medicine [EP/L015838/1]
- AstraZeneca
- Diamond Light Source
- Defense Science and Technology Laboratory
- Evotec
- GlaxoSmithKline
- Novartis
- Pfizer
- Janssen
- Syngenta
- UCB
- Vertex
- Takeda
- Swiss Cancer League [KFS-4702-02-2019]
- AbbVie
- Bayer Pharma AG
- Boehringer Ingelheim
- Canada Foundation for Innovation
- Eshelman Institute for Innovation
- Genome Canada
- Innovative Medicines Initiative (EU/EFPIA) [ULTRA-DD) [115766]
- Merck Co.
- Novartis Pharma AG
- Ontario Ministry of Economic Development and Innovation
- Sao Paulo Research Foundation-FAPESP
- Wellcome Trust [092809/Z/10/Z]
- Swiss National Science Foundation (SNF) [31003A_176161] Funding Source: Swiss National Science Foundation (SNF)
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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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