[HTML][HTML] Advances in covalent drug discovery

L Boike, NJ Henning, DK Nomura - Nature Reviews Drug Discovery, 2022 - nature.com
Covalent drugs have been used to treat diseases for more than a century, but tools that
facilitate the rational design of covalent drugs have emerged more recently. The purposeful …

E3 ligase ligands for PROTACs: how they were found and how to discover new ones

T Ishida, A Ciulli - … Advancing the Science of Drug Discovery, 2021 - journals.sagepub.com
Bifunctional degrader molecules, also called proteolysis-targeting chimeras (PROTACs), are
a new modality of chemical tools and potential therapeutics to understand and treat human …

Emerging and re-emerging warheads for targeted covalent inhibitors: applications in medicinal chemistry and chemical biology

M Gehringer, SA Laufer - Journal of medicinal chemistry, 2018 - ACS Publications
Targeted covalent inhibitors (TCIs) are designed to bind poorly conserved amino acids by
means of reactive groups, the so-called warheads. Currently, targeting noncatalytic cysteine …

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 …

Open-air alkylation reactions in photoredox-catalyzed DNA-encoded library synthesis

JP Phelan, SB Lang, J Sim, S Berritt… - Journal of the …, 2019 - ACS Publications
DNA-encoded library (DEL) technology is a powerful tool commonly used by the
pharmaceutical industry for the identification of compounds with affinity to biomolecular …

The symbiotic relationship between drug discovery and organic chemistry

OO Grygorenko, DM Volochnyuk… - … A European Journal, 2020 - Wiley Online Library
All pharmaceutical products contain organic molecules; the source may be a natural product
or a fully synthetic molecule, or a combination of both. Thus, it follows that organic chemistry …

[HTML][HTML] Recent advances in selective and irreversible covalent ligand development and validation

T Zhang, JM Hatcher, M Teng, NS Gray, M Kostic - Cell chemical biology, 2019 - cell.com
Some of the most widely used drugs, such as aspirin and penicillin, are covalent drugs.
Covalent binding can improve potency, selectivity, and duration of the effects, but the …

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 …

10 years into the resurgence of covalent drugs

E De Vita - Future Medicinal Chemistry, 2021 - Taylor & Francis
In the first decade of targeted covalent inhibition, scientists have successfully reversed the
previous trend that had impeded the use of covalent inhibition in drug development …