Sunday, January 16, 2022

A Series of Pyrazole Analogs Binding to KRASG12C as Potential Cancer Treatment

Gerard Rosse

ACS Med. Chem. Lett. 2022, 13, 1, 11–12

https://doi.org/10.1021/acsmedchemlett.1c00643

The compounds of this patent application represent a potential treatment for cancer characterized by KRAS, HRAS, and NRAS GC12 mutation. The compounds have the ability to inhibit the G12C mutant of KRAS, HRAS, and NRAS via the formation of an irreversible bond to cysteine 12. The irreversible binding locks KRAS in an inactivate state and disrupts downstream signaling.



4-Oxo-β-lactams as Covalent Inhibitors of the Mitochondrial Intramembrane Protease PARL

Shanping Ji, Kathrin Bach, Vijay Madhav Miriyala, Jan Dohnálek, Miguel Riopedre-Fernandez, Martin Lepšík, Merel van de Plassche, Roeland Van...