Source: BEFREE

Gene Disease Score gda Association Type Original DB Sentence supporting the association PMID PMID Year
Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 Biomarker BEFREE BRAF and MEK1/2 inhibitors are effective in melanoma but resistance inevitably develops. 31727888

2019

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 GeneticVariation BEFREE Combinatorial inhibition of MEK1/2 and CDK4/6 is currently undergoing clinical investigation in NRAS-mutant melanoma. 30819666

2019

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 Biomarker 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

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 Biomarker BEFREE A MEK1/2 inhibitor, binimetinib is promising as a therapeutic agent for malignant melanoma with N-RAS mutation. 31129802

2019

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 Biomarker 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

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 Biomarker BEFREE Together, these pathways provide a way to activate MAPK signaling downstream of BRAF and MEK1 inhibitors, which are commonly used to treat melanoma. 30543563

2019

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 Biomarker BEFREE ERK1 is the immediate downstream target of MEK1/2, which is druggable with trametinib, an approved therapeutic for melanoma. 30804427

2019

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 Biomarker BEFREE Recent clinical and therapeutic success with RAF and MEK1/2 inhibitors has revolutionized the existing treatment schemes for previously incurable cancers like melanomas. 31662208

2019

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 Biomarker BEFREE While the role of the BRAF-MEK1/2-ERK1/2 pathway in melanoma is well established, the involvement of mitogen-activated protein kinases MEK5-ERK5 remains poorly explored. 29483645

2018

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 Biomarker 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

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 Biomarker BEFREE The mitogen-activated extracellular signal-regulated kinase 1/2 (MEK1/2) inhibitor trametinib has shown promising therapeutic effects on melanoma, but its efficacy on colorectal cancer (CRC) is limited. 28756770

2017

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 GeneticVariation 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

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 Biomarker BEFREE Targeting BMK1 Impairs the Drug Resistance to Combined Inhibition of BRAF and MEK1/2 in Melanoma. 28387310

2017

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 Biomarker BEFREE phase II and III clinical trials demonstrated modest anti- tumor activity of Binimetinib (MEK162) - a potent allosteric inhibitor of MEK1 and MEK2- in patients with advanced NRAS mutant melanoma. 28919996

2017

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 Biomarker BEFREE Corrigendum: Targeting BMK1 Impairs the Drug Resistance to Combined Inhibition of BRAF and MEK1/2 in Melanoma. 28548101

2017

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 Biomarker 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

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 GeneticVariation BEFREE Cobimetinib: inhibiting MEK1/2 in BRAF V600-mutant melanoma. 28112278

2016

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 GeneticVariation BEFREE Taken together, our data indicate that preexisting MEK1(P124) mutations are associated with a reduced response to BRAF inhibitor therapy and identify a subset of patients with BRAF-mutant melanoma likely to benefit from combination therapies involving MEK or ERK inhibitors. 25370473

2015

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 GeneticVariation BEFREE This MEK1(T55delins) (RT) mutation could be traced back to a fraction of the pre-treatment lesion and not only provided protection against vemurafenib but also promoted local invasion of transplanted melanomas. 26105199

2015

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 Biomarker BEFREE PI3'-kinase inhibition forestalls the onset of MEK1/2 inhibitor resistance in BRAF-mutated melanoma. 25472943

2015

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 AlteredExpression BEFREE Single treatment of BRAF mutant melanoma cell lines with vemurafenib or dabrafenib (BRAF inhibitors) alone or in combination with trametinib (MEK1/2 inhibitor) resulted in overexpression of Mcl-1. 26497853

2015

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 GeneticVariation 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

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 GeneticVariation BEFREE Our data confirming that MEK2(C125S), but not the synonymous MEK1(C121S) protein, confers resistance to combination therapy highlight the functional differences between these kinases and the preponderance of MEK2 mutations in combination therapy-resistant melanomas. 25452114

2014

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 GeneticVariation BEFREE We found that the acquired MEK1-C121S mutation in BRAF-V600E mutant melanoma conferred resistance to both vemurafenib and selumetinib but not E6201. 24448821

2014

Entrez Id: 5604
Gene Symbol: MAP2K1
MAP2K1
CUI: C0025202
Disease: melanoma
melanoma
0.700 Biomarker 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