[HTML][HTML] Dynamic reprogramming of the kinome in response to targeted MEK inhibition in triple-negative breast cancer

JS Duncan, MC Whittle, K Nakamura, AN Abell… - Cell, 2012 - cell.com
… suggested a kinase inhibitor combination therapy that produced … We used RNAi for each
kinase in the MAPK pathway to … coincides with the reactivation of RAF-MEK-ERK signaling. …

ERK mutations confer resistance to mitogen-activated protein kinase pathway inhibitors

EM Goetz, M Ghandi, DJ Treacy, N Wagle… - Cancer research, 2014 - AACR
… involves reactivation of the MAPK (RAF/MEK/ERK) pathway … that are sensitive to MAP kinase
pathway inhibitors. These cells … MEK inhibitor trametinib (GSK1120212), or the combination

[HTML][HTML] MAPK pathway in melanoma part II—secondary and adaptive resistance mechanisms to BRAF inhibition

T Amaral, T Sinnberg, F Meier, C Krepler… - European journal of …, 2017 - Elsevier
… or BRAFV600E-MEK MUT , which lead to MAPK pathway reactivation. Cells with
combination-drug … We recently described both MAPK pathway reactivation and PI3K pathway

Combined inhibition of MEK and nuclear ERK translocation has synergistic antitumor activity in melanoma cells

R Arafeh, K Flores, A Keren-Paz, G Maik-Rachline… - Scientific reports, 2017 - nature.com
… shown to result in either reactivation of the ERK1/2 signaling, failure to effectively deactivate
ERK1/2, or activate alternative signaling pathways that overcome the inhibition of ERK1/2. …

A Cell-Based MAPK Reporter Assay Reveals Synergistic MAPK Pathway Activity Suppression by MAPK Inhibitor Combination in BRAF-Driven Pediatric Low-Grade …

D Usta, R Sigaud, JL Buhl, F Selt, V Marquardt… - Molecular cancer …, 2020 - AACR
… Screening of a MAPKi library revealed MEK inhibitors as the class inhibiting the pathway
with the lowest IC 50 s, followed by ERK and next-generation RAF inhibitors. Combination

Combined BRAF, EGFR, and MEK Inhibition in Patients with BRAFV600E-Mutant Colorectal Cancer

RB Corcoran, T André, CE Atreya, JHM Schellens… - Cancer discovery, 2018 - AACR
… RTK-mediated reactivation of the MAPK pathway … , combined inhibition of BRAF, EGFR, and
MEK is hypothesized to prevent adaptive feedback reactivation and maintain MAPK pathway

Inhibition of the Ras/Raf/MEK/ERK and RET kinase pathways with the combination of the multikinase inhibitor sorafenib and the farnesyltransferase inhibitor tipifarnib …

DS Hong, ME Cabanillas, J Wheler… - The Journal of …, 2011 - academic.oup.com
… In conclusion, we demonstrate that combining sorafenib and … suggests that this combination
warrants further investigation … of multiple pathways by the two-drug combination contributes …

Mitogen-activated protein kinase (MEK) inhibitors to treat melanoma alone or in combination with other kinase inhibitors

E Faghfuri, S Nikfar, K Niaz, MA Faramarzi… - Expert Opinion on …, 2018 - Taylor & Francis
… in tumor microenvironment could reactivate the MAPK/ERK and PI3K/AKT pathways.
Resistance is also acquired through reactivation of the MAPK/ERK pathway, which can happen …

MAP Kinase Pathway Alterations in BRAF-Mutant Melanoma Patients with Acquired Resistance to Combined RAF/MEK Inhibition

N Wagle, EM Van Allen, DJ Treacy, DT Frederick… - Cancer discovery, 2014 - AACR
… melanoma to date result in reactivation of MEK/ERK signaling (5–11). … combined targeting
of BRAF and MEK. In a phase I/II trial of combined dabrafenib and tremetinib, this combination

Identifying genotype-dependent efficacy of single and combined PI3K-and MAPK-pathway inhibition in cancer

ML Sos, S Fischer, R Ullrich, M Peifer… - Proceedings of the …, 2009 - National Acad Sciences
… The effect of MAPK signaling inhibition is compatible with stable disease, and thus again,
reactivation of the PI3K signaling might limit the single agent activity of MEK inhibition. …