KRAS mutation: from undruggable to druggable in cancer
L Huang, Z Guo, F Wang, L Fu - Signal transduction and targeted …, 2021 - nature.com
Cancer is the leading cause of death worldwide, and its treatment and outcomes have been
dramatically revolutionised by targeted therapies. As the most frequently mutated oncogene …
dramatically revolutionised by targeted therapies. As the most frequently mutated oncogene …
Targeting KRAS mutant cancers: from druggable therapy to drug resistance
C Zhu, X Guan, X Zhang, X Luan, Z Song, X Cheng… - Molecular cancer, 2022 - Springer
Abstract Kirsten Rat Sarcoma Viral Oncogene Homolog (KRAS) is the most frequently
mutated oncogene, occurring in a variety of tumor types. Targeting KRAS mutations with …
mutated oncogene, occurring in a variety of tumor types. Targeting KRAS mutations with …
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 …
Comutations and KRASG12C Inhibitor Efficacy in Advanced NSCLC
MV Negrao, HA Araujo, G Lamberti, AJ Cooper… - Cancer discovery, 2023 - AACR
Molecular modifiers of KRASG12C inhibitor (KRASG12Ci) efficacy in advanced KRAS G12C-
mutant NSCLC are poorly defined. In a large unbiased clinicogenomic analysis of 424 …
mutant NSCLC are poorly defined. In a large unbiased clinicogenomic analysis of 424 …
The KRAS-G12C inhibitor: activity and resistance
Although it has long been deemed “undruggable”, with the development of drugs specifically
binding the KRAS-G12C mutant protein, clinical trials that directly inhibit oncogenic RAS …
binding the KRAS-G12C mutant protein, clinical trials that directly inhibit oncogenic RAS …
Scribble mis-localization induces adaptive resistance to KRAS G12C inhibitors through feedback activation of MAPK signaling mediated by YAP-induced MRAS
Y Adachi, R Kimura, K Hirade, S Yanase, Y Nishioka… - Nature Cancer, 2023 - nature.com
Tumor cells evade targeted drugs by rewiring their genetic and epigenetic networks. Here,
we identified that inhibition of MAPK signaling rapidly induces an epithelial-to-mesenchymal …
we identified that inhibition of MAPK signaling rapidly induces an epithelial-to-mesenchymal …
Tumor-selective activity of RAS-GTP inhibition in pancreatic cancer
UN Wasko, J Jiang, TC Dalton, A Curiel-Garcia… - Nature, 2024 - nature.com
Broad-spectrum RAS inhibition holds the potential to benefit roughly a quarter of human
cancer patients whose tumors are driven by RAS mutations1, 2. RMC-7977 is a highly …
cancer patients whose tumors are driven by RAS mutations1, 2. RMC-7977 is a highly …
Oncogenic KRAS blockade therapy: renewed enthusiasm and persistent challenges
Across a broad range of human cancers, gain-of-function mutations in RAS genes (HRAS,
NRAS, and KRAS) lead to constitutive activity of oncoproteins responsible for tumorigenesis …
NRAS, and KRAS) lead to constitutive activity of oncoproteins responsible for tumorigenesis …
Kras oncogene ablation prevents resistance in advanced lung adenocarcinomas
M Salmón, R Álvarez-Díaz… - The Journal of …, 2023 - Am Soc Clin Investig
KRASG12C inhibitors have revolutionized the clinical management of patients with KRAS
G12C-mutant lung adenocarcinoma. However, patient exposure to these inhibitors leads to …
G12C-mutant lung adenocarcinoma. However, patient exposure to these inhibitors leads to …
Treatment strategies for KRAS-mutated non-small-cell lung cancer
Simple Summary KRAS plays an important role in transmitting signals from growth factors on
the outside of the cell to the cell nucleus. It regulates cell proliferation, growth, and survival …
the outside of the cell to the cell nucleus. It regulates cell proliferation, growth, and survival …