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

A multicenter, open-label, first-in-human study of TYRA-200 in advanced intrahepatic cholangiocarcinoma and other solid tumors with activating FGFR2 gene alterations (SURF201).

Jordi Rodon Ahnert ,  Sameek Roychowdhury ,  Haley Ellis ,  Fernando F. Blanco ,  Timothy Burn ,  Jennifer Michelle Davis ,  Alex Balcer ,  ...