MEK1 mutations confer resistance to MEK and B-RAF inhibition
CM Emery, KG Vijayendran… - Proceedings of the …, 2009 - National Acad Sciences
… P124L allele in resistance to MEK inhibition, we examined the effects of MEK inhibition on ex
vivo … In this study, we used a systematic approach that combined random mutagenesis and …
vivo … In this study, we used a systematic approach that combined random mutagenesis and …
[HTML][HTML] AurkA inhibitors enhance the effects of B-RAF and MEK inhibitors in melanoma treatment
E Caputo, R Miceli, ML Motti, R Taté… - Journal of translational …, 2014 - Springer
… combined B-RAF/AurkA inhibition for B-RAF mutated melanomas and MEK/AurkA inhibitor
combination for patients without B-RAF … RAF, MEK and AurkA inhibitor triple drug combination …
combination for patients without B-RAF … RAF, MEK and AurkA inhibitor triple drug combination …
[HTML][HTML] CRAF mutations in lung cancer can be oncogenic and predict sensitivity to combined type II RAF and MEK inhibition
A Noeparast, P Giron, A Noor, R Bahadur Shahi… - Oncogene, 2019 - nature.com
… type II RAF inhibitors and a MEK inhibitor led to a stronger ERK pathway inhibition and growth
… with CRAF oncogene dependency to the combination of type II RAF and MEK inhibition. …
… with CRAF oncogene dependency to the combination of type II RAF and MEK inhibition. …
RAF dimer inhibition enhances the antitumor activity of MEK inhibitors in K‐RAS mutant tumors
X Yuan, Z Tang, R Du, Z Yao, SH Cheung… - Molecular …, 2020 - Wiley Online Library
… We observed enhanced antitumor efficacy for RAF dimer and MEK inhibitor combination, …
reports suggesting RAF dimer or pan-RAF inhibitor in combination with MEK inhibitor may be a …
reports suggesting RAF dimer or pan-RAF inhibitor in combination with MEK inhibitor may be a …
Rational combination therapy with PARP and MEK inhibitors capitalizes on therapeutic liabilities in RAS mutant cancers
… Thus, the ability of mutant RAS to suppress FOXO3a and its reversal by MEK inhibitors … and
MEK inhibitors in RAS mutant tumors. The rational combination of PARP and MEK inhibitors …
MEK inhibitors in RAS mutant tumors. The rational combination of PARP and MEK inhibitors …
[HTML][HTML] Acquired resistance to BRAF inhibition can confer cross-resistance to combined BRAF/MEK inhibition
K Gowrishankar, S Snoyman, GM Pupo… - Journal of investigative …, 2012 - Elsevier
… targeting of BRAF and its downstream target MAPK/ERK kinase (MEK) may … of combination
BRAF and MEK inhibition, we generated melanoma cell clones resistant to the BRAF inhibitor …
BRAF and MEK inhibition, we generated melanoma cell clones resistant to the BRAF inhibitor …
Combined BRAF and MEK Inhibition With Dabrafenib and Trametinib in BRAF V600–Mutant Colorectal Cancer
RB Corcoran, CE Atreya, GS Falchook… - Journal of clinical …, 2015 - ascopubs.org
… Our study suggests that dual MAPK pathway blockade with the BRAF inhibitor dabrafenib
and the MEK inhibitor trametinib can lead to meaningful clinical benefit in a subset of patients …
and the MEK inhibitor trametinib can lead to meaningful clinical benefit in a subset of patients …
The clinical development of MEK inhibitors
Y Zhao, AA Adjei - Nature reviews Clinical oncology, 2014 - nature.com
… of each pathway individually, a recent study combined PD0325901 with a dual PI3K and
mTOR inhibitor, PF-04691502, in a multiarm phase I study; 71 however, toxic effects precluded …
mTOR inhibitor, PF-04691502, in a multiarm phase I study; 71 however, toxic effects precluded …
Exploiting allosteric properties of RAF and MEK inhibitors to target therapy-resistant tumors driven by oncogenic BRAF signaling
… A rationally designed combination of RAF and MEK inhibitors based on their conformation
selectivity achieved increased efficacy and a high therapeutic index when used to target …
selectivity achieved increased efficacy and a high therapeutic index when used to target …
Therapeutic potential of MEK inhibition in acute myelogenous leukemia: rationale for “vertical” and “lateral” combination strategies
MR Ricciardi, MC Scerpa, P Bergamo… - Journal of molecular …, 2012 - Springer
… RAF activation in response to MEK inhibition [27] … combined MEK and RAF inhibition provide
unequivocal evidence of a striking pro-apoptotic synergism of such a “vertical” combination …
unequivocal evidence of a striking pro-apoptotic synergism of such a “vertical” combination …