Sunday, May 28, 2023

Covalent drug discovery using sulfur(VI) fluoride exchange warheads

Huang Huang, Lyn H. Jones

Expert Opinion on Drug Discovery, 2023

https://doi.org/10.1080/17460441.2023.2218642

      Covalent drug discovery has traditionally focused on targeting cysteine, but the amino acid is often absent in protein binding sites. This review makes the case to move beyond cysteine labeling using sulfur (VI) fluoride exchange (SuFEx) chemistry to expand the druggable proteome.
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N-Acyl-N-alkyl/aryl Sulfonamide Chemistry Assisted by Proximity for Modification and Covalent Inhibition of Endogenous Proteins in Living Systems

Tomonori Tamura and Itaru Hamachi Accounts of Chemical Research 2025 58 (1), 87-100 DOI: 10.1021/acs.accounts.4c00628 Selective chemical mo...