Cytotoxic activity of KRAS inhibitors in combination with chemotherapeutics

G Hamilton, A Plangger - Expert Opinion on Drug Metabolism & …, 2021 - Taylor & Francis
… not identified common hits for KRAS mutant cancer cells that … combination with mutation-specific
and pan-KRAS inhibitors. … that promotes RTKKRAS signaling in KRAS-driven cancers …

EGFR Blockade Reverts Resistance to KRASG12C Inhibition in Colorectal Cancer

V Amodio, R Yaeger, P Arcella, C Cancelliere… - Cancer discovery, 2020 - AACR
… We and others previously reported that acquired KRAS mutations … We reasoned that KRAS
inhibitors could have clinical … on RTK signaling across KRAS G12C -mutant tumors can be …

SHP2 is required for growth of KRAS-mutant non-small-cell lung cancer in vivo

S Mainardi, A Mulero-Sánchez, A Prahallad… - Nature medicine, 2018 - nature.com
inhibition as an unexpected vulnerability of KRAS-mutant … kinase kinase (MEK) inhibition in
KRAS-mutant lung and colon … as a readout of RTK activation in a panel of KRAS-mutant lung, …

Efforts to develop KRAS inhibitors

M Holderfield - Cold Spring Harbor Perspectives …, 2018 - perspectivesinmedicine.cshlp.org
… of KRAS mutations in human cancers and the lack of effective treatments for patients ranks
KRAS … for decades to identify small molecule inhibitors of oncogenic KRAS proteins, but little …

Small-molecule inhibitors and degraders targeting KRAS-driven cancers

S Hyun, D Shin - International Journal of Molecular Sciences, 2021 - mdpi.com
… of KRAS inhibitors, successful therapies for KRAS mutation-induced cancers, including the
direct inhibition of the activity of KRAS and inhibition of downstream KRAS signaling, via the …

Mechanisms of response and tolerance to active RAS inhibition in KRAS-mutant NSCLC

HA Araujo, X Pechuan-Jorge, T Zhou, MT Do… - Cancer …, 2024 - aacrjournals.org
… On-treatment feedback reactivation of the RAS-MAPK pathway, as a result of synthesis
and GTP-loading of new KRASG12C and/or RTK-driven activation of wild-type RAS, (KRAS, …

Discovery and characterization of the potent, allosteric SHP2 inhibitor GDC-1971 for the treatment of RTK/RAS driven tumors

B Williams, A Taylor, O Orozco, C Owen, E Kelley… - Cancer Research, 2022 - AACR
KRAS G12C inhibitorsKRAS G12C covalent inhibitor GDC-6036 resulted in significant
regressions at doses well below those required for single agent activity in a KRAS G12C-mutant

KRAS mutation in pancreatic cancer

J Luo - Seminars in oncology, 2021 - Elsevier
KRAS mutant cancer, MAPK and PI3K pathway inhibitors have not demonstrated significant
clinical activity in patients with KRAS mutant … the feedback inhibition of RTK signaling [42]. In …

[HTML][HTML] KRAS inhibition in non–small cell lung cancer: Past failures, new findings and upcoming challenges

F Passiglia, U Malapelle, M Del Re, L Righi… - European Journal of …, 2020 - Elsevier
KRAS mutations detection in the Italian real-word scenario, summarises the biological basis
of KRAS inhibition … Recent preclinical data identified RTK-mediated feedback reactivation of …

Mutant KRAS-driven cancers depend on PTPN11/SHP2 phosphatase

DA Ruess, GJ Heynen, KJ Ciecielski, J Ai… - Nature medicine, 2018 - nature.com
… /MEK inhibition is not only restricted to the KRAS mutant but is … As an integrator of RTK–RAS
signaling downstream of almost … only in RTK-driven tumors but also in KRAS-mutant tumors. …