[HTML][HTML] Paradox breaker BRAF inhibitors have comparable potency and MAPK pathway reactivation to encorafenib in BRAF mutant colorectal cancer

OJ Pickles, A Drozd, L Tee, AD Beggs, GW Middleton - Oncotarget, 2020 - ncbi.nlm.nih.gov
… resulting in MEK-ERK pathway reactivation. … pathway reactivation, we reasoned that
PLX8394 may be a more effective BRAF inhibitor in BRAF mutant CRC for use in combination

Targeting the ERK signaling pathway in melanoma

P Savoia, P Fava, F Casoni, O Cremona - International journal of …, 2019 - mdpi.com
… The discovery of the role of the RAS/RAF/MEK/ERK pathway … The combination therapy with
MEK inhibitors is an excellent … due to the paradoxical reactivation of the MAPK pathway. The …

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

R Barbosa, LA Acevedo, R Marmorstein - Molecular Cancer Research, 2021 - AACR
… in combination with either BRAF inhibitor dabrafenib or vemurafenib against BRAF V600E
cancer cell lines (119). The tolerance to this combination in … induce pathway reactivation and …

Inverse correlation of STAT3 and MEK signaling mediates resistance to RAS pathway inhibition in pancreatic cancer

NS Nagathihalli, JA Castellanos, P Lamichhane… - Cancer research, 2018 - AACR
… the AREG–EGFR–MEK–STAT3 pathway to overcome therapeutic resistance associated
with RAS pathway reactivation in PDAC. In addition, combined MEKi and STAT3i inhibits CSCs …

JNK Pathway Activation Modulates Acquired Resistance to EGFR/HER2–Targeted Therapies

S Manole, EJ Richards, AS Meyer - Cancer research, 2016 - AACR
… a combined experimental- and statistical modeling–based approach to identify a set of
pathway reactivation … to examine the nature of combination Mek and JNK inhibition on viability (…

Sensitivity of KRAS-mutant colorectal cancers to combination therapy that cotargets MEK and CDK4/6

EK Ziemke, JS Dosch, JD Maust, A Shettigar… - Clinical Cancer …, 2016 - AACR
… activity of MEK and further impair its reactivation by CRAF by … to combine MEK and PI3K
pathway inhibitors in the clinic only to be met with significant toxicity issues. Combination of MEK

The ERK cascade inhibitors: Towards overcoming resistance

G Maik-Rachline, R Seger - Drug resistance updates, 2016 - Elsevier
… that can reactivate ERK and other survival-related pathways. … reactivation of MEK by RAF
in vemurafenib-resistant cells (see below), initiated new strategy of combining RAF and MEK

Fibroblast growth factor receptor 3‐mediated reactivation of ERK signaling promotes head and neck squamous cancer cell insensitivity to MEK inhibition

MJ Ban, HK Byeon, YJ Yang, S An, JW Kim… - Cancer …, 2018 - Wiley Online Library
MEK in HNSCC, as MEK/ERK reactivation inevitably occurs. We assessed the effects of
combining … ERK 1/2-pathway reactivation during acquired resistance has led to the identification …

A transcriptional MAPK Pathway Activity Score (MPAS) is a clinically relevant biomarker in multiple cancer types

MC Wagle, D Kirouac, C Klijn, B Liu, S Mahajan… - NPJ precision …, 2018 - nature.com
pathway hyperactivation in tumors, 7 in some instances, these drugs have demonstrated
therapeutic benefit alone or in combination … and in sensitivity to MEK pathway inhibitors (ie, MV), …

[HTML][HTML] Combined MEK and Pi3′-kinase inhibition reveals synergy in targeting thyroid cancer in vitro and in vivo

O ElMokh, D Ruffieux-Daidié, MA Roelli, A Stooss… - Oncotarget, 2017 - ncbi.nlm.nih.gov
… , we propose the combination of a MEK inhibitor and a Pi3′-… due to reactivation of the ERK
signaling pathway via various … (Pi3′-kinase) pathways by inhibiting the mutated enzymes …