Exceptions to a long-held rule against chemically bonding to biological targets are powering new cancer medicines, finds Andy Extance
https://www.chemistryworld.com/feature/covalent-inhibitor-drugs/2500494.article
A blog highlighting recent publications in the area of covalent modification of proteins, particularly relating to covalent-modifier drugs. @CovalentMod on Twitter, @covalentmod@mstdn.science on Mastodon, and @covalentmod.bsky.social on BlueSky
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Discovery and Optimization of a Covalent AKR1C3 Inhibitor
R. Justin Grams, Wesley J. Wolfe, Robert J. Seal, James Veccia, and Ku-Lung Hsu Journal of Medicinal Chemistry 2025 DOI: 10.1021/acs.jmedch...
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DOI Ansgar Oberheide, Maxime van den Oetelaar, Jakob Scheele, Jan Borggräfe, Semmy Engelen, Michael Sattler, Christian Ottmann, ...
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Özge Ünsal, Z. Selin Bacaksiz, Vladislav Khamraev, Vittorio Montanari, Martin Beinborn, and Krishna Kumar ACS Chemical Biology 2024 DOI: ...
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Klett, T., Schwer, M., Ernst, L. N., Engelhardt, M. U., Jaag, S. J., Masberg, B., … Boeckler, F. M. Drug Design, Development and Therapy, 20...