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.
at

Discovery and Optimization of a WRN Helicase Inhibitor Series through Structure-Guided Drug Design from a Covalent Fragment Binding Insight

Momar Toure * ; Xin Cindy Yan; Yonghong Bai; Brian A. Sosa-Alvarado; Cen Gao; Theresa Baker; Erin Brophy; John R. Butler; Yuchen Yuan; Micha...