Diverse alterations associated with resistance to KRAS (G12C) inhibition

Y Zhao, YR Murciano-Goroff, JY Xue, A Ang, J Lucas… - Nature, 2021 - nature.com
Inactive state-selective KRAS (G12C) inhibitors,,,,,,–demonstrate a 30–40% response rate
and result in approximately 6-month median progression-free survival in patients with lung …

Silent mutations reveal therapeutic vulnerability in RAS Q61 cancers

Y Kobayashi, C Chhoeu, J Li, KS Price, LA Kiedrowski… - Nature, 2022 - nature.com
RAS family members are the most frequently mutated oncogenes in human cancers.
Although KRAS (G12C)-specific inhibitors show clinical activity in patients with cancer …

[HTML][HTML] The KRAS-G12C inhibitor: activity and resistance

J Liu, R Kang, D Tang - Cancer gene therapy, 2022 - nature.com
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 …

Resistance looms for KRAS G12C inhibitors and rational tackling strategies

J Zhang, J Zhang, Q Liu, XX Fan, ELH Leung… - Pharmacology & …, 2022 - Elsevier
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 …

Resistance to KRAS G12C inhibition in non-small cell lung cancer

A Di Federico, I Ricciotti, V Favorito… - Current Oncology …, 2023 - Springer
Abstract Purpose of Review Although the recent development of direct KRASG12C inhibitors
(G12Ci) has improved outcomes in KRAS mutant cancers, responses occur only in a fraction …

Overcoming KRAS-Mutant Lung Cancer

J Luo, J Ostrem, B Pellini, D Imbody, Y Stern… - American Society of …, 2022 - ascopubs.org
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 …

[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 …

[HTML][HTML] Pan-KRAS inhibitor disables oncogenic signalling and tumour growth

D Kim, L Herdeis, D Rudolph, Y Zhao, J Böttcher… - Nature, 2023 - nature.com
KRAS is one of the most commonly mutated proteins in cancer, and efforts to directly inhibit
its function have been continuing for decades. The most successful of these has been the …

Clinical Acquired Resistance to KRASG12C Inhibition through a Novel KRAS Switch-II Pocket Mutation and Polyclonal Alterations Converging on RAS–MAPK …

N Tanaka, JJ Lin, C Li, MB Ryan, J Zhang… - Cancer discovery, 2021 - AACR
Mutant-selective KRASG12C inhibitors, such as MRTX849 (adagrasib) and AMG 510
(sotorasib), have demonstrated efficacy in KRAS G12C-mutant cancers, including non–small …

[HTML][HTML] 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 …