Back to the bench? MEK and ERK inhibitors for the treatment of KRAS mutant lung adenocarcinoma

J Kohler, M Catalano… - Current Medicinal …, 2018 - ingentaconnect.com
… state of MEK and ERK inhibitors in pre-clinical models and in human clinical trials for … MEK
inhibitor to date [75], single agent MEK inhibitors have only marginal activity in KRAS mutant

KRAS dimerization impacts MEK inhibitor sensitivity and oncogenic activity of mutant KRAS

C Ambrogio, J Köhler, ZW Zhou, H Wang, R Paranal… - Cell, 2018 - cell.com
… wild-type KRAS-dependent fitness of human and murine KRAS mutant LUAD … MEK inhibition.
These effects are abrogated when wild-type KRAS is replaced by KRAS D154Q , a mutant

MEK inhibitors for the treatment of NRAS mutant melanoma

S Sarkisian, D Davar - Drug Design, Development and Therapy, 2018 - Taylor & Francis
… /MEK inhibitors in the treatment of this disease. We describe the recent development of
the selective MEK inhibitor … with AKT inhibitor MK-2206 in KRAS mutant cancers, Citation101 …

KRAS mutation as a resistance mechanism to BRAF/MEK inhibition in NSCLC

M Niemantsverdriet, E Schuuring, A Ter Elst… - Journal of Thoracic …, 2018 - jto.org
… V600E/KRAS p.G12V double-positive clone rather than a therapy-induced KRAS mutation.
Because the patient received both BRAF and MEK inhibition, the double mutant clone may …

KRAS mutation: from undruggable to druggable in cancer

L Huang, Z Guo, F Wang, L Fu - Signal transduction and targeted …, 2021 - nature.com
… hope of drugging KRAS. In this review, the latest research progress on KRAS, the characteristics
of KRAS mutations, the relationship between the KRAS mutations and tumour immunity, …

[HTML][HTML] Efficacy of the combination of MEK and CDK4/6 inhibitors in vitro and in vivo in KRAS mutant colorectal cancer models

MS Lee, TL Helms, N Feng, J Gay, QE Chang, F Tian… - Oncotarget, 2016 - ncbi.nlm.nih.gov
… Consequently, we hypothesized that the combination of a CDK4/6 inhibitor and a MEK
inhibitor would have synergistic antitumor activity in vitro and in vivo in KRAS mutant CRC. …

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells

O Kauko, CM O'Connor, E Kulesskiy… - Science translational …, 2018 - science.org
inhibitor sensitivity of KRAS-mutant lung cancer cells To evaluate the global relevance of
PP2A activity for kinase inhibitor responses in human KRAS-mutant … (22) in KRAS-mutant A549 …

Epithelial-to-Mesenchymal Transition Defines Feedback Activation of Receptor Tyrosine Kinase Signaling Induced by MEK Inhibition in KRAS-Mutant Lung Cancer

H Kitai, H Ebi, S Tomida, KV Floros, H Kotani, Y Adachi… - Cancer discovery, 2016 - AACR
… Herein, we report that MEK inhibition leads to distinct activation of RTKs in KRAS-mutant lung
… In epithelial-like KRAS-mutant cancer cells, MEK inhibition upregulates ERBB3, which in …

Key roles of EMT for adaptive resistance to MEK inhibitor in KRAS mutant lung cancer

H Kitai, H Ebi - Small GTPases, 2017 - Taylor & Francis
… of KRAS, blocking this pathway with MEK inhibitors is … of MAPK signal following MEK inhibition
by multiple feedback … signaling following MEK inhibition in KRAS mutant lung cancer. In …

SHP2 inhibition overcomes RTK-mediated pathway reactivation in KRAS-mutant tumors treated with MEK inhibitors

H Lu, C Liu, R Velazquez, H Wang, LM Dunkl… - Molecular cancer …, 2019 - AACR
… cell lines, by measuring the reduction of phospho-MEK adaptive induction after … MEK
inhibitors led to enhanced antiproliferative activity and MAPK pathway suppression in KRAS-mutant