Molecular pathways: adaptive kinome reprogramming in response to targeted inhibition of the BRAF–MEK–ERK pathway in cancer
GL Johnson, TJ Stuhlmiller, SP Angus… - Clinical Cancer …, 2014 - AACR
… but MEK2 escaped inhibition, allowing reactivation of ERK. Thus, MEK2 selectively …
inhibition by allosteric MEK inhibitors. The mechanism for selective MEK2 escape from inhibition …
inhibition by allosteric MEK inhibitors. The mechanism for selective MEK2 escape from inhibition …
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
… Like MEK inhibitors, GDC-0994 has broad activity in numerous … inhibition is likewise limited
by pathway reactivation. We therefore explored the concept of dual node suppression of MEK …
by pathway reactivation. We therefore explored the concept of dual node suppression of MEK …
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
… in a large panel (n = 34) of KRAS-mutant cell lines, by measuring the reduction of phospho-MEK
… SHP2 and MEK inhibitors led to enhanced antiproliferative activity and MAPK pathway …
… SHP2 and MEK inhibitors led to enhanced antiproliferative activity and MAPK pathway …
Enhanced inhibition of ERK signaling by a novel allosteric MEK inhibitor, CH5126766, that suppresses feedback reactivation of RAF activity
N Ishii, N Harada, EW Joseph, K Ohara, T Miura… - Cancer research, 2013 - AACR
… pathway inhibition by standard MEK inhibitors. CH5126766 represents a new type of MEK
inhibitor that causes MEK … reactivation of RAF by conventional allosteric MEK inhibitors is …
inhibitor that causes MEK … reactivation of RAF by conventional allosteric MEK inhibitors is …
MEK inhibitor resistance mechanisms and recent developments in combination trials
E Kun, YTM Tsang, CW Ng, DM Gershenson… - Cancer treatment …, 2021 - Elsevier
… is the reactivation of multiple RTKs upstream of the MAPK pathway responsible for … pathways
by which they can promote cell signaling, and reactivation of RTKs following MEK inhibition …
by which they can promote cell signaling, and reactivation of RTKs following MEK inhibition …
[HTML][HTML] Resistance to combination BRAF and MEK inhibition in metastatic melanoma: Where to next?
… /MEK inhibitors (BRAF/MEKi) for BRAF V600 -mutant metastatic melanoma, and we explore
the three major effectors of BRAF/MEK inhibitor … pathway reactivation as the mechanism of …
the three major effectors of BRAF/MEK inhibitor … pathway reactivation as the mechanism of …
[HTML][HTML] Concurrent MEK targeted therapy prevents MAPK pathway reactivation during BRAFV600E targeted inhibition in a novel syngeneic murine glioma model
S Grossauer, K Koeck, NE Murphy, ID Meyers… - Oncotarget, 2016 - ncbi.nlm.nih.gov
… MEK inhibitor trametinib delivered by oral gavage daily suppressed MAPK pathway more …
Compared with either agent alone, combined BRAF V600E and MEK inhibitor treatment …
Compared with either agent alone, combined BRAF V600E and MEK inhibitor treatment …
COT drives resistance to RAF inhibition through MAP kinase pathway reactivation
… MEK inhibitors in combination can override resistance to single agents 15 . We therefore
reasoned that combined RAF/MEK inhibition … the importance of this pathway in B-RAF(V600E) …
reasoned that combined RAF/MEK inhibition … the importance of this pathway in B-RAF(V600E) …
Combination therapies to inhibit the RAF/MEK/ERK pathway in melanoma: we are not done yet
GA McArthur - Frontiers in oncology, 2015 - frontiersin.org
… MEK inhibition and frequent reactivation of RAF/MEK/ERK signaling as a mechanism of
resistance to BRAF inhibitor … BRAF and MEK inhibition. Because the combination of BRAF and …
resistance to BRAF inhibitor … BRAF and MEK inhibition. Because the combination of BRAF and …
The clinical development of MEK inhibitors
Y Zhao, AA Adjei - Nature reviews Clinical oncology, 2014 - nature.com
… coexisting oncogenic pathways could negate the activity of MEK inhibitors, specifically the
PI3K–AKT pathway, which … As reactivation of MEK–MAPK signalling has been proposed as a …
PI3K–AKT pathway, which … As reactivation of MEK–MAPK signalling has been proposed as a …
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