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 …
Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C
A Weiss, E Lorthiois, L Barys, KS Beyer… - Cancer discovery, 2022 - AACR
Covalent inhibitors of KRASG12C have shown antitumor activity against
advanced/metastatic KRASG12C-mutated cancers, though resistance emerges and …
advanced/metastatic KRASG12C-mutated cancers, though resistance emerges and …
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 …
Targeting Krasg12c‐mutant cancer with a mutation‐specific inhibitor
JG Christensen, P Olson, T Briere… - Journal of internal …, 2020 - Wiley Online Library
The RAS genes, which include H, N, and KRAS, comprise the most frequently mutated
family of oncogenes in cancer. Mutations in KRAS–such as the G12C mutation–are found in …
family of oncogenes in cancer. Mutations in KRAS–such as the G12C mutation–are found in …
Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor
X Wang, S Allen, JF Blake, V Bowcut… - Journal of medicinal …, 2021 - ACS Publications
KRASG12D, the most common oncogenic KRAS mutation, is a promising target for the
treatment of solid tumors. However, when compared to KRASG12C, selective inhibition of …
treatment of solid tumors. However, when compared to KRASG12C, selective inhibition of …
Anti-tumor efficacy of a potent and selective non-covalent KRASG12D inhibitor
J Hallin, V Bowcut, A Calinisan, DM Briere, L Hargis… - Nature medicine, 2022 - nature.com
Recent progress in targeting KRASG12C has provided both insight and inspiration for
targeting alternative KRAS mutants. In this study, we evaluated the mechanism of action and …
targeting alternative KRAS mutants. In this study, we evaluated the mechanism of action and …
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 …
KRasG12C inhibitors in clinical trials: a short historical perspective
KRas is the most frequently mutated oncogene in human cancer, and even 40 years after
the initial discovery of Ras oncogenes in 1982, no approved drug directly targets Ras in Ras …
the initial discovery of Ras oncogenes in 1982, no approved drug directly targets Ras in Ras …
The path to the clinic: a comprehensive review on direct KRASG12C inhibitors
The RAS oncogene is both the most frequently mutated oncogene in human cancer and the
first confirmed human oncogene to be discovered in 1982. After decades of research, in …
first confirmed human oncogene to be discovered in 1982. After decades of research, in …
Cell Type–specific Adaptive Signaling Responses to KRASG12C Inhibition
HS Solanki, EA Welsh, B Fang, V Izumi, L Darville… - Clinical Cancer …, 2021 - AACR
Purpose: Covalent inhibitors of KRASG12C specifically target tumors driven by this form of
mutant KRAS, yet early studies show that bypass signaling drives adaptive resistance …
mutant KRAS, yet early studies show that bypass signaling drives adaptive resistance …
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