DNA-encoded chemical libraries: a comprehensive review with succesful stories and future challenges

A Gironda-Martínez, EJ Donckele… - ACS Pharmacology & …, 2021 - ACS Publications
DNA-encoded chemical libraries (DELs) represent a versatile and powerful technology
platform for the discovery of small-molecule ligands to protein targets of biological and …

DNA-encoded chemistry: drug discovery from a few good reactions

PR Fitzgerald, BM Paegel - Chemical reviews, 2020 - ACS Publications
Click chemistry, proposed nearly 20 years ago, promised access to novel chemical space by
empowering combinatorial library synthesis with a “few good reactions”. These click …

[HTML][HTML] The expanding reaction toolkit for DNA-encoded libraries

RJ Fair, RT Walsh, CD Hupp - Bioorganic & Medicinal Chemistry Letters, 2021 - Elsevier
Over the past decade, DNA-encoded libraries (DELs) have emerged as a leading platform
for small molecule drug discovery among pharmaceutical companies, biotech companies …

Abiotic peptides as carriers of information for the encoding of small-molecule library synthesis

SL Rössler, NM Grob, SL Buchwald, BL Pentelute - Science, 2023 - science.org
Encoding small-molecule information in DNA has been leveraged to accelerate the
discovery of ligands for therapeutic targets such as proteins. However, oligonucleotide …

DNA-encoded chemistry technology yields expedient access to SARS-CoV-2 Mpro inhibitors

S Chamakuri, S Lu, MN Ucisik… - Proceedings of the …, 2021 - National Acad Sciences
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has killed more than 4
million humans globally, but there is no bona fide Food and Drug Administration–approved …

DNA-encoded libraries (DELs): a review of on-DNA chemistries and their output

Y Shi, Y Wu, J Yu, W Zhang, C Zhuang - RSC advances, 2021 - pubs.rsc.org
A DNA-encoded library is a collection of small molecules covalently linked to DNA that has
unique information about the identity and the structure of each library member. A DNA …

High-power screening (HPS) empowered by DNA-encoded libraries

YK Sunkari, VK Siripuram, TL Nguyen… - Trends in …, 2022 - cell.com
The world is totally dependent on medications. As science progresses, new, better, and
cheaper drugs are needed more than ever. The pharmaceutical industry has been …

Discovery and characterization of bromodomain 2–specific inhibitors of BRDT

Z Yu, AF Ku, JL Anglin, R Sharma… - Proceedings of the …, 2021 - National Acad Sciences
Bromodomain testis (BRDT), a member of the bromodomain and extraterminal (BET)
subfamily that includes the cancer targets BRD2, BRD3, and BRD4, is a validated …

Synthesis of functionalized triazoles on DNA via azide-acetonitrile “click” reaction

X Fang, T Zhang, W Fang, G Zhang, Y Li, Y Li - Organic Letters, 2023 - ACS Publications
Triazoles are privileged structural motifs that are embedded in a number of molecules with
interesting biological activities. In this work, we developed a practical and general synthetic …

Multiplexed CuAAC Suzuki–Miyaura labeling for tandem activity-based chemoproteomic profiling

J Cao, LM Boatner, HS Desai, NR Burton… - Analytical …, 2021 - ACS Publications
Mass-spectrometry-based chemoproteomics has enabled the rapid and proteome-wide
discovery of functional and potentially'druggable'hotspots in proteins. While numerous …