Strategies for developing DNA-encoded libraries beyond binding assays

Y Huang, Y Li, X Li - Nature Chemistry, 2022 - nature.com
DNA-encoded chemical libraries (DELs) have emerged as a powerful technology in drug
discovery. The wide adoption of DELs in the pharmaceutical industry and the rapid …

DNA-encoded chemistry: enabling the deeper sampling of chemical space

RA Goodnow Jr, CE Dumelin, AD Keefe - Nature Reviews Drug …, 2017 - nature.com
DNA-encoded chemical library technologies are increasingly being adopted in drug
discovery for hit and lead generation. DNA-encoded chemistry enables the exploration of …

Combinatorial chemistry in drug discovery

R Liu, X Li, KS Lam - Current opinion in chemical biology, 2017 - Elsevier
Several combinatorial methods have been developed to create focused or diverse chemical
libraries with a wide range of linear or macrocyclic chemical molecules: peptides, non …

Chemical space of DNA-encoded libraries: Miniperspective

RM Franzini, C Randolph - Journal of medicinal chemistry, 2016 - ACS Publications
In recent years, DNA-encoded chemical libraries (DECLs) have attracted considerable
attention as a potential discovery tool in drug development. Screening encoded libraries …

DNA-encoded chemical libraries: a selection system based on endowing organic compounds with amplifiable information

D Neri, RA Lerner - Annual review of biochemistry, 2018 - annualreviews.org
The discovery of organic ligands that bind specifically to proteins is a central problem in
chemistry, biology, and the biomedical sciences. The encoding of individual organic …

[HTML][HTML] 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 …

Recording binding information directly into DNA-Encoded libraries using terminal deoxynucleotidyl transferase

LA Schneider, B Sauter, K Dagher… - Journal of the American …, 2023 - ACS Publications
Terminal deoxynucleotidyl transferase (TdT) is an unusual DNA polymerase that adds
untemplated dNTPs to 3′-ends of DNA. If a target protein is expressed as a TdT fusion and …

Antibody–drug conjugates and small molecule–drug conjugates: opportunities and challenges for the development of selective anticancer cytotoxic agents …

G Casi, D Neri - Journal of medicinal chemistry, 2015 - ACS Publications
Conventional cancer chemotherapy heavily relies on the use of cytotoxic agents, which
typically do not preferentially localize at the tumor site and cause toxicity to normal organs …

Versatile protein recognition by the encoded display of multiple chemical elements on a constant macrocyclic scaffold

Y Li, R De Luca, S Cazzamalli, F Pretto, D Bajic… - Nature …, 2018 - nature.com
In nature, specific antibodies can be generated as a result of an adaptive selection and
expansion of lymphocytes with suitable protein binding properties. We attempted to mimic …

DNA‐Encoded Libraries: Aryl Fluorosulfonates as Versatile Electrophiles Enabling Facile On‐DNA Suzuki, Sonogashira, and Buchwald Reactions

H Xu, F Ma, N Wang, W Hou, H Xiong, F Lu… - Advanced …, 2019 - Wiley Online Library
Using (hetero) aryl fluorosulfonates as versatile electrophiles, facile on‐DNA cross‐coupling
reactions of Suzuki, Sonogashira, and Buchwald are reported here. Notably, all of these …