Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.2c01120
Abstract: Activating mutations in KRAS are the most frequent oncogenic alterations in cancer. The oncogenic hotspot position 12, located at the lip of the switch II pocket, offers a covalent attachment point for KRASG12C inhibitors. To… read more here.
Keywords: switch pocket; krasg12c inhibitor; pocket; vivo active ... See more keywords
Abstract 3448: Discovery of HYP-2A,a 2nd- generation KRASG12C inhibitor exhibits potent in vivo efficacy in drug resistant tumor models
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-3448
Abstract: Although activating mutations in KRAS are well recognized as a hallmark of cancer, KRAS was considered an undruggable target for over 30 years after its discovery, due to the intrinsic characteristics of KRAS proteins. The… read more here.
Keywords: hyp; krasg12c inhibitor; efficacy; krasg12c ... See more keywords
Validation of an LC-MS/MS method for the determination of sotorasib, a KRASG12C inhibitor, in human plasma.
Sign Up to like & getrecommendations! Published in 2022 at "Bioanalysis"
DOI: 10.4155/bio-2022-0173
Abstract: Background: Sotorasib (AMG 510) is a first-in-class KRASG12C inhibitor that received accelerated US FDA approval in 2021 for the treatment of patients with KRASG12C-mutated locally advanced or metastatic non-small-cell lung cancer. Method: An LC-MS/MS method… read more here.
Keywords: human plasma; krasg12c inhibitor; method; determination sotorasib ... See more keywords