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A PROTAC for KRAS G12C Degradation
Targeted Degradation of Oncogenic KRASG12C by VHL-Recruiting PROTACs.
ACS Cent. Sci. 2020;
KRas is one of the most promising cancer drug targets, but targeting it has been a challenge. Crews and co-workers employed covalent KRas G12C inhibitors for the development of PROTACS that allowed for its targeted degradation.
A solvent-exposed site in the clinical drug candidate MRTX849 was identified and used for conjugation to a linker and a VHL ligand to yield the PROTAC LC-2.
20 October 2020 (online)
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