Clinical Acquired Resistance to KRASG12C Inhibition through a Novel KRAS Switch-II Pocket Mutation and Polyclonal Alterations Converging on RAS–MAPK�…
Mutant-selective KRASG12C inhibitors, such as MRTX849 (adagrasib) and AMG 510
(sotorasib), have demonstrated efficacy in KRAS G12C-mutant cancers, including non–small�…
(sotorasib), have demonstrated efficacy in KRAS G12C-mutant cancers, including non–small�…
More to the RAS Story: KRASG12C Inhibition, Resistance Mechanisms, and Moving Beyond KRASG12C
CD Lietman, ML Johnson, F McCormick…�- American Society of�…, 2022 - ascopubs.org
Despite the discovery of RAS oncogenes in human tumor DNA 40 years ago, the
development of effective targeted therapies directed against RAS has lagged behind those�…
development of effective targeted therapies directed against RAS has lagged behind those�…
[HTML][HTML] Resistance to KRASG12C Inhibitors in Non-Small Cell Lung Cancer
JB Blaquier, AF Cardona, G Recondo�- Frontiers in Oncology, 2021 - frontiersin.org
KRAS mutations are one of the most prevalent oncogenic alterations in cancer. Until
recently, drug development targeting KRAS did not convey clinical benefits to patients�…
recently, drug development targeting KRAS did not convey clinical benefits to patients�…
Mechanisms of Resistance to KRASG12C-Targeted Therapy
NS Akhave, AB Biter, DS Hong�- Cancer discovery, 2021 - AACR
KRAS mutations are among the most common drivers of human carcinogenesis, and are
associated with poor prognosis and an aggressive disease course. With the advent of�…
associated with poor prognosis and an aggressive disease course. With the advent of�…
[HTML][HTML] Overcoming resistance to drugs targeting KRASG12C mutation
D Jiao, S Yang�- The Innovation, 2020 - cell.com
Activating KRAS mutations are present in 25% of human cancer. Although oncogenic Ras
was deemed" undruggable" in the past, recent efforts led to the development of�…
was deemed" undruggable" in the past, recent efforts led to the development of�…
Acquired Resistance to KRASG12C Inhibition in Cancer
MM Awad, S Liu, II Rybkin, KC Arbour…�- …�England Journal of�…, 2021 - Mass Medical Soc
Background Clinical trials of the KRAS inhibitors adagrasib and sotorasib have shown
promising activity in cancers harboring KRAS glycine-to-cysteine amino acid substitutions at�…
promising activity in cancers harboring KRAS glycine-to-cysteine amino acid substitutions at�…
The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients
J Hallin, LD Engstrom, L Hargis, A Calinisan, R Aranda…�- Cancer discovery, 2020 - AACR
Despite decades of research, efforts to directly target KRAS have been challenging.
MRTX849 was identified as a potent, selective, and covalent KRASG12C inhibitor that�…
MRTX849 was identified as a potent, selective, and covalent KRASG12C inhibitor that�…
[HTML][HTML] Rapid idiosyncratic mechanisms of clinical resistance to KRAS G12C inhibition
YS Tsai, MG Woodcock, SH Azam…�- The Journal of�…, 2022 - Am Soc Clin Investig
BACKGROUND The KRAS proto-oncogene is among the most frequently mutated genes in
cancer, yet for 40 years it remained an elusive therapeutic target. Recently, allosteric�…
cancer, yet for 40 years it remained an elusive therapeutic target. Recently, allosteric�…
Overcoming KRAS-Mutant Lung Cancer
More than 50 years after the discovery of RAS family proteins, which harbor the most
common activating mutations in cancer, the US Food and Drug Administration approved the�…
common activating mutations in cancer, the US Food and Drug Administration approved the�…
Resistance looms for KRAS G12C inhibitors and rational tackling strategies
KRAS mutations are one of the most frequent activating alterations in carcinoma. Recent
efforts have witnessed a revolutionary strategy for KRAS G12C inhibitors with exhibiting�…
efforts have witnessed a revolutionary strategy for KRAS G12C inhibitors with exhibiting�…