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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Peptide-based covalent inhibitor of tubulin detyrosination promotes mesenchymal-to-epithelial transition in lung cancer cells

Hathaichanok Impheng, Ghislain Gillard, Nuttanid Numnoi, and Krzysztof Rogowski  PNAS   123   ( 1 )   e2514990123 https://doi.org/10.1073/pn...