[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 …
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 …
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 …
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 …
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 …
discovery for hit and lead generation. DNA-encoded chemistry enables the exploration of …
Open-air alkylation reactions in photoredox-catalyzed DNA-encoded library synthesis
DNA-encoded library (DEL) technology is a powerful tool commonly used by the
pharmaceutical industry for the identification of compounds with affinity to biomolecular …
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 …
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
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 …
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 …
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 …
previous trend that had impeded the use of covalent inhibition in drug development …