melanoma
|
0.700 |
CausalMutation
|
disease |
CGI |
|
|
|
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 |
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 |
Biomarker
|
disease |
LHGDN |
Surprisingly, MEK1 and ERK1/2 activities were restored in integrin alphav-negative melanoma cells by suppression of p53, whereas concomitant block of MEK1 induced apoptosis.
|
15557124 |
2004 |
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 |
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 |
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 |
GeneticVariation
|
disease |
CLINVAR |
MEK1 mutations confer resistance to MEK and B-RAF inhibition.
|
19915144 |
2009 |
melanoma
|
0.700 |
GeneticVariation
|
disease |
BEFREE |
We thus report for the first time a low prevalence of MEK1 mutations in melanoma and colon cancer.
|
19411838 |
2009 |
melanoma
|
0.700 |
CausalMutation
|
disease |
CLINVAR |
MEK1 mutations confer resistance to MEK and B-RAF inhibition.
|
19915144 |
2009 |
melanoma
|
0.700 |
GeneticVariation
|
disease |
BEFREE |
One such mutation, MEK1(P124L), was identified in a resistant metastatic focus that emerged in a melanoma patient treated with AZD6244.
|
19915144 |
2009 |
melanoma
|
0.700 |
CausalMutation
|
disease |
CLINVAR |
COT drives resistance to RAF inhibition through MAP kinase pathway reactivation.
|
21107320 |
2010 |
melanoma
|
0.700 |
CausalMutation
|
disease |
CLINVAR |
Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling.
|
21383288 |
2011 |
melanoma
|
0.700 |
GeneticVariation
|
disease |
BEFREE |
Screening a larger cohort of individuals with melanoma revealed the presence of recurring somatic MAP2K1 and MAP2K2 mutations, which occurred at an overall frequency of 8%.
|
22197931 |
2011 |
melanoma
|
0.700 |
Biomarker
|
disease |
CTD_human |
Screening a larger cohort of individuals with melanoma revealed the presence of recurring somatic MAP2K1 and MAP2K2 mutations, which occurred at an overall frequency of 8%.
|
22197931 |
2011 |
melanoma
|
0.700 |
CausalMutation
|
disease |
CLINVAR |
Screening a larger cohort of individuals with melanoma revealed the presence of recurring somatic MAP2K1 and MAP2K2 mutations, which occurred at an overall frequency of 8%.
|
22197931 |
2011 |
melanoma
|
0.700 |
CausalMutation
|
disease |
CLINVAR |
Preexisting MEK1 exon 3 mutations in V600E/KBRAF melanomas do not confer resistance to BRAF inhibitors.
|
22588879 |
2012 |
melanoma
|
0.700 |
GeneticVariation
|
disease |
BEFREE |
Thus, activating MEK1 exon 3 mutations identified herein and concurrent with V600E/KBRAF do not cause BRAFi resistance in melanoma.
|
22588879 |
2012 |
melanoma
|
0.700 |
CausalMutation
|
disease |
CLINVAR |
Melanoma genome sequencing reveals frequent PREX2 mutations.
|
22622578 |
2012 |
melanoma
|
0.700 |
Biomarker
|
disease |
BEFREE |
To compare the efficacy and tolerability of the mitogen-activated protein (MAP)/extracellular signal-regulated (ERK) kinase (MEK) 1/2 inhibitor selumetinib versus temozolomide in chemotherapy-naive patients with unresectable stage III/IV melanoma.
|
22048237 |
2012 |
melanoma
|
0.700 |
GeneticVariation
|
disease |
CLINVAR |
Phase II trial of MEK inhibitor selumetinib (AZD6244, ARRY-142886) in patients with BRAFV600E/K-mutated melanoma.
|
23444215 |
2013 |
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 |
GeneticVariation
|
disease |
CLINVAR |
Pharmacodynamic effects and mechanisms of resistance to vemurafenib in patients with metastatic melanoma.
|
23569304 |
2013 |
melanoma
|
0.700 |
Biomarker
|
disease |
BEFREE |
The purpose of this study was to determine the response rate (RR) for the selective, allosteric MEK1/MEK2 inhibitor trametinib (GSK1120212), in patients with metastatic BRAF-mutant melanoma.
|
23248257 |
2013 |
melanoma
|
0.700 |
CausalMutation
|
disease |
CLINVAR |
Pharmacodynamic effects and mechanisms of resistance to vemurafenib in patients with metastatic melanoma.
|
23569304 |
2013 |