Synfacts 2020; 16(11): 1353
DOI: 10.1055/s-0040-1706368
Chemistry in Medicine and Biology

A PROTAC for KRAS G12C Degradation

Rezensent(en):
Dirk Trauner
,
Johannes Morstein
Bond MJ, Chu L, Nalawansha DA, Li K, Crews CM. * Yale University, New Haven, USA
Targeted Degradation of Oncogenic KRASG12C by VHL-Recruiting PROTACs.

ACS Cent. Sci. 2020;
6: 1367-1375
DOI: 10.1021/acscentsci.0c00411.
 

Significance

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.


#

Comment

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.


#
#

Publikationsverlauf

Publikationsdatum:
20. Oktober 2020 (online)

© 2020. Thieme. All rights reserved

Georg Thieme Verlag KG
Rüdigerstraße 14, 70469 Stuttgart, Germany