[HTML][HTML] KRAS mutation: from undruggable to druggable in cancer

L Huang, Z Guo, F Wang, L Fu - Signal transduction and targeted …, 2021 - nature.com
… were associated with genomic aberrations that were associated with the RAS/RTK pathway
79 . … Selective inhibitors targeting specific KRAS mutations are urgently needed to effectively …

Targeting KRAS mutant lung cancer: light at the end of the tunnel

M Drosten, M Barbacid - Molecular oncology, 2022 - Wiley Online Library
… effect of RTK inhibition may be … inhibition could be effective in patients with KRAS mutant
lung tumors [[114]]. Interestingly, CDK4/6 inhibitors also synergized with KRAS G12C inhibitors

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
… upstream signaling with RTK inhibitors that increase the activity of KRAS G12C … RTK
signaling to KRAS. Accordingly, SHP2 inhibitors are active in cancers driven by KRAS mutations

[HTML][HTML] Drugging KRAS: current perspectives and state-of-art review

K Parikh, G Banna, SV Liu, A Friedlaender… - Journal of hematology & …, 2022 - Springer
inhibitors that block mutant KRAS G12C were successfully developed and sotorasib was the
first KRAS G12C inhibitor to … We also discuss the relationship between KRAS mutations and …

SOS1 and KSR1 modulate MEK inhibitor responsiveness to target resistant cell populations based on PI3K and KRAS mutation status

BR Daley, HM Vieira, C Rao… - Proceedings of the …, 2023 - National Acad Sciences
… with KRAS Q61 and/or PIK3CA mutations were … KRAS mutant cell lines in both PIK3CA-mutated
and PIK3CA wild-type cancers. Our findings demonstrate that vertical inhibition of RTK/…

[HTML][HTML] Genome-wide CRISPR-cas9 knockout screening identifies GRB7 as a driver for MEK inhibitor resistance in KRAS mutant colon cancer

C Yu, D Luo, J Yu, M Zhang, X Zheng, G Xu, J Wang… - Oncogene, 2022 - nature.com
… Here, we found that GRB7 maintained RTK signaling via PLK1 in CRC cells with KRAS
mutations. GRB7 overexpression promoted the cytoplasmic localization of PLK1, which might be …

Breaking oncogene addiction: getting RTK/RAS-mutated cancers off the SOS

E Sheffels, RL Kortum - Journal of Medicinal Chemistry, 2021 - ACS Publications
… survival in KRAS mutant cancer cells, (… inhibitor of proximal RTK signaling may be a common
therapeutic strategy to enhance RTK inhibitor efficacy and treat cancers dependent on RTK

[HTML][HTML] Escaping KRAS: gaining autonomy and resistance to KRAS inhibition in KRAS mutant cancers

Y Adachi, R Kimura, K Hirade, H Ebi - Cancers, 2021 - mdpi.com
… lung cancer, EMT has been shown to play a defining role in the feedback reactivation of
RTK signaling following MEK inhibition. In epithelial-like cells, this feedback was mediated by …

[HTML][HTML] Direct Targeting KRAS Mutation in Non-Small Cell Lung Cancer: Focus on Resistance

D Reita, L Pabst, E Pencreach, E Guérin, L Dano… - Cancers, 2022 - mdpi.com
KRAS mutations favor the active form with inhibition of GTPAse activity. KRAS mutations are
… by a release of upstream feedback inhibition of RTK which bypass KRAS G12C inhibition by …

Overcoming KRAS-Mutant Lung Cancer

J Luo, J Ostrem, B Pellini, D Imbody, Y Stern… - American Society of …, 2022 - ascopubs.org
KRAS mutations impart insensitivity to inhibitors of upstream … mutations within KRAS and
associated RTK and MAPK signaling molecules, acquired resistance to KRAS G12C inhibitors