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.

Fragment-Based Covalent Targeting of Lysines at the Allosteric Latch Site of SHP2.

  Vincenzo Di Lorenzo , Noémi Csorba , Renáta Szabó , Levente Kollár , Yvette Roske , Ivan Rand̵elović , Krisztina Balázs , Tibor Vikt...