Tuesday, October 15, 2024

New electrophiles targeting thiols in a reversible covalent manner

Xingyu Ma,   Manyi Xu,   Fengge Wang,  Tingting Hu,  Xinyuan Chena  and  Chong-Jing Zhang

Chem. Commun., 2024
DOI
https://doi.org/10.1039/D4CC04612A

Reversible covalent electrophiles with the advantages of both reversible and covalent interactions receive much attention in the fields of chemical biology and medicinal chemistry. Here, we report two electron-deficient olefins activated by amide and ester, amide-substituted acrylamide and methyl ester-substituted acrylamide, targeting thiols in a reversible covalent manner.

A covalent inhibitor targeting Cys-349 of LIMK1 confers selectivity over LIMK2

Jon B. Patteson,  Ioannis Manolaridis, Mee Ra Hong,  Jennifer M. Johnston, Samaneh Mesbahi-Vasey,  Michael C. Gregory ,Daniel V. Iwamoto Joh...