[HTML][HTML] Synergistic inhibition of MEK and reciprocal feedback networks for targeted intervention in malignancy

Y Li, Q Dong, Y Cui - Cancer Biology & Medicine, 2019 - ncbi.nlm.nih.gov
Abstract The RAS-RAF-MEK-ERK signaling pathway (MAPK signaling pathway) plays a
significant role in multiple pathological behaviors and is most frequently dysregulated in …

Beyond single pathway inhibition: MEK inhibitors as a platform for the development of pharmacological combinations with synergistic anti-leukemic effects

M Milella, CM Precupanu, C Gregorj… - Current …, 2005 - ingentaconnect.com
The MEK/MAPK signaling module is a key integration point along signal transduction
cascades that regulate cell growth, survival, and differentiation, and is aberrantly activated in …

The MEK/ERK network as a therapeutic target in human cancer

R Barbosa, LA Acevedo, R Marmorstein - Molecular Cancer Research, 2021 - AACR
Abstract The RAS–RAF–MEK–ERK pathway is the most well-studied of the MAPK cascades
and is critical for cell proliferation, differentiation, and survival. Abnormalities in regulation …

[PDF][PDF] Allosteric MEK1/2 inhibitors for the treatment of cancer: an overview

L McDermott, C Qin - J Drug Res Dev, 2015 - researchgate.net
Abstract The RAS-RAF-MEK-ERK mitogen activated protein kinase (MAPK) pathway is a
driver behind key cellular processes such as gene transcription, cellular proliferation …

Targeting aberrant RAS/RAF/MEK/ERK signaling for cancer therapy

U Degirmenci, M Wang, J Hu - Cells, 2020 - mdpi.com
The RAS/RAF/MEK/ERK (MAPK) signaling cascade is essential for cell inter-and intra-
cellular communication, which regulates fundamental cell functions such as growth, survival …

Allosteric modulators of MEK1: drug design and discovery

J Shang, S Lu, Y Jiang, J Zhang - Chemical Biology & Drug …, 2016 - Wiley Online Library
Mitogen‐activated protein kinase kinase (MAPKK, MEK) mediates signal transduction,
controlling cell proliferation and survival. MEK occupies a key downstream position in the …

Combined MEK and ERK inhibition overcomes therapy-mediated pathway reactivation in RAS mutant tumors

M Merchant, J Moffat, G Schaefer, J Chan, X Wang… - PloS one, 2017 - journals.plos.org
Mitogen-activated protein kinase (MAPK) pathway dysregulation is implicated in> 30% of all
cancers, rationalizing the development of RAF, MEK and ERK inhibitors. While BRAF and …

Targeting the RAF–MEK–ERK pathway in cancer therapy

C Montagut, J Settleman - Cancer letters, 2009 - Elsevier
The clinical success of selective kinase inhibitors, such as imatinib and erlotinib, as
therapeutic agents for several human cancers has prompted substantial interest in the …

The clinical development of MEK inhibitors

Y Zhao, AA Adjei - Nature reviews Clinical oncology, 2014 - nature.com
Aberrant activation of the RAS–RAF–MEK–ERK1/2 pathway occurs in more than 30% of
human cancers. As part of this pathway, MEK1 and MEK2 have crucial roles in …

MEK1/2 inhibitors: molecular activity and resistance mechanisms

PK Wu, JI Park - Seminars in oncology, 2015 - Elsevier
Aberrant activation of the three-layered protein kinase cascade, Raf/MEK/ERK, is often
detected in human cancer, which is mainly attributed to the oncogenic alterations of RAF, or …