melanoma
|
0.700 |
CausalMutation
|
disease |
CGI |
|
|
|
melanoma
|
0.700 |
Biomarker
|
disease |
BEFREE |
MEK1/2 and BRAF<sup>V600E</sup> inhibitors are used to treat BRAF<sup>V600E</sup>-positive melanoma, with other cancers under evaluation.
|
28986383 |
2017 |
melanoma
|
0.700 |
Biomarker
|
disease |
BEFREE |
A MEK1/2 inhibitor, binimetinib is promising as a therapeutic agent for malignant melanoma with N-RAS mutation.
|
31129802 |
2019 |
melanoma
|
0.700 |
AlteredExpression
|
disease |
BEFREE |
Anthrax lethal toxin-sensitive melanoma cell lines and normal cells had higher phospho-MEK1/2 levels than anthrax lethal toxin-resistant melanoma cell lines and normal tissue types.
|
16170021 |
2005 |
melanoma
|
0.700 |
Biomarker
|
disease |
BEFREE |
Biomarker results from a phase II study of MEK1/2 inhibitor binimetinib (MEK162) in patients with advanced <i>NRAS</i>- or <i>BRAF</i>-mutated melanoma.
|
30956763 |
2019 |
melanoma
|
0.700 |
Biomarker
|
disease |
BEFREE |
BRAF and MEK1/2 inhibitors are effective in melanoma but resistance inevitably develops.
|
31727888 |
2019 |
melanoma
|
0.700 |
GeneticVariation
|
disease |
BEFREE |
Cobimetinib: inhibiting MEK1/2 in BRAF V600-mutant melanoma.
|
28112278 |
2016 |
melanoma
|
0.700 |
GeneticVariation
|
disease |
BEFREE |
Combinatorial inhibition of MEK1/2 and CDK4/6 is currently undergoing clinical investigation in NRAS-mutant melanoma.
|
30819666 |
2019 |
melanoma
|
0.700 |
GeneticVariation
|
disease |
BEFREE |
Consistent with these observations, pharmacological inhibition of BRAF(V600E) or MEK1/2 in human melanoma cells (using PLX4720 and CI-1040 respectively) led to a striking elevation of BIM expression.
|
18715233 |
2008 |
melanoma
|
0.700 |
Biomarker
|
disease |
BEFREE |
Corrigendum: Targeting BMK1 Impairs the Drug Resistance to Combined Inhibition of BRAF and MEK1/2 in Melanoma.
|
28548101 |
2017 |
melanoma
|
0.700 |
CausalMutation
|
disease |
CLINVAR |
COT drives resistance to RAF inhibition through MAP kinase pathway reactivation.
|
21107320 |
2010 |
melanoma
|
0.700 |
Biomarker
|
disease |
BEFREE |
Coupling MEK1/2 inhibitors with B-Raf inhibitors is more effective in treating such melanomas and dual therapy is now the standard of care.
|
30118796 |
2018 |
melanoma
|
0.700 |
GeneticVariation
|
disease |
CLINVAR |
Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors.
|
23614898 |
2013 |
melanoma
|
0.700 |
CausalMutation
|
disease |
CLINVAR |
Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling.
|
21383288 |
2011 |
melanoma
|
0.700 |
Biomarker
|
disease |
BEFREE |
ERK1 is the immediate downstream target of MEK1/2, which is druggable with trametinib, an approved therapeutic for melanoma.
|
30804427 |
2019 |
melanoma
|
0.700 |
Biomarker
|
disease |
BEFREE |
FABP7 mRNA and protein level is down-regulated following treatment of melanoma cell lines with a PKC activator (PMA) or MEK1 inhibitor (PD98059).
|
18826602 |
2008 |
melanoma
|
0.700 |
Biomarker
|
disease |
BEFREE |
Furthermore, recently identified ERK1/2-inducing mutations in MEK1 and MEK2 (MEK1/2) MAPK genes in melanoma confer resistance to emerging therapeutic MEK inhibitors, underscoring the challenges facing direct kinase inhibition in cancer.
|
23603816 |
2013 |
melanoma
|
0.700 |
Biomarker
|
disease |
BEFREE |
Furthermore, we found that melanoma cell integrin alphav was required for MAPK kinase (MEK) 1 and extracellular signal-regulated kinase (ERK)1/2 activity in 3D-collagen, whereas inhibition of MEK1 activity induced apoptosis.
|
15557124 |
2004 |
melanoma
|
0.700 |
GeneticVariation
|
disease |
BEFREE |
In patients with BRAF-mutated melanoma specific inhibitors of BRAF<sup>V600E</sup> and MEK1/2 frequently induce initial tumor reduction, frequently followed by relapse.
|
28720543 |
2017 |
melanoma
|
0.700 |
GeneticVariation
|
disease |
BEFREE |
In recent years, intracellular signal transduction via RAS-RAF-MEK-ERK has been successfully targeted in new treatment approaches for melanoma using small molecule inhibitors against activated BRAF (V600E mutation) and activated MEK1/2.
|
25654738 |
2015 |
melanoma
|
0.700 |
Biomarker
|
disease |
BEFREE |
It inhibited colorectal cancer and melanoma cell proliferation much more effectively than its negative control MS432N (<b>24</b>), and its effect was phenocopied by MEK1/2 knockdown.
|
31730343 |
2019 |
melanoma
|
0.700 |
GeneticVariation
|
disease |
CLINVAR |
MEK1 mutations confer resistance to MEK and B-RAF inhibition.
|
19915144 |
2009 |
melanoma
|
0.700 |
CausalMutation
|
disease |
CLINVAR |
MEK1 mutations confer resistance to MEK and B-RAF inhibition.
|
19915144 |
2009 |
melanoma
|
0.700 |
CausalMutation
|
disease |
CLINVAR |
Melanoma genome sequencing reveals frequent PREX2 mutations.
|
22622578 |
2012 |
melanoma
|
0.700 |
AlteredExpression
|
disease |
LHGDN |
Mutation of B-Raf in human choroidal melanoma cells mediates cell proliferation and transformation through the MEK/ERK pathway.
|
12917419 |
2003 |