Property Summary

NCBI Gene PubMed Count 298
Grant Count 428
R01 Count 280
Funding $32,172,359.92
PubMed Score 808.57
PubTator Score 555.59

Knowledge Summary

Patent (54,927)

Expression

  Differential Expression (13)

Disease log2 FC p
Multiple myeloma 1.710 0.001
astrocytic glioma -1.700 0.003
ependymoma -1.800 0.008
oligodendroglioma -1.500 0.000
glioblastoma multiforme -1.200 0.000
medulloblastoma -2.000 0.000
atypical teratoid / rhabdoid tumor -1.400 0.000
medulloblastoma, large-cell -2.100 0.000
primitive neuroectodermal tumor -1.500 0.000
subependymal giant cell astrocytoma -2.129 0.019
Pick disease -1.400 0.001
ovarian cancer 1.300 0.000
dermatomyositis 1.100 0.005

Synonym

Accession Q02750 MAP kinase kinase 1
Symbols CFC3
MEK1
MKK1
MAPKK1
PRKMK1

Gene

PDB

4MNE   1S9J   2P55   3DV3   3DY7   3E8N   3EQB   3EQC   3EQD   3EQF   3EQG   3EQH   3EQI   3MBL   3ORN   3OS3   3PP1   3SLS   3V01   3V04   3VVH   3W8Q   3WIG   3ZLS   3ZLW   3ZLX   3ZLY   3ZM4   4AN2   4AN3   4AN9   4ANB   4ARK   4LMN   4U7Z   4U80   4U81   5BX0   5EYM  

  TechDev Info (1)

Gary Johnson Kinome profile via MIB/MS Technology

MLP Assay (3)

AID Type Active / Inconclusive / Inactive Description
1732 confirmatory 4 / 10 / 58 Assay for Inhibitors of the ERK Signaling Pathway using a Homogeneous Screening Assay: MEK Inhibition
1982 other 0 / 0 / 0 Kinase inhibition selectivity assay for compound SID-48409448
588725 other 0 / 0 / 1 Late stage counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): Radioactivity-based biochemical assay to identify modulators of a panel of 48 kinases

Gene RIF (230)

PMID Text
27098723 the purpose of this paper was to investigate MAPK downstream signalling molecules in Natural killer cell phenotypes from Chronic Fatigue Syndrome/Myalgic Encephalomyelitis patients.
26858456 Endocytosis separates EGF receptors from endogenous fluorescently labeled HRas and diminishes receptor signaling to MAP kinases in endosomes.
26825960 Specific inhibition of BRAF oncogene, MEK or p38 signaling was associated with decreases in DIO3 expression in papillary thyroid cancer cells
26625317 Data show that mitogen-activated protein kinase kinases MEK1/2 inhibitor pimasertib (MEKI) sensitized the cells to apoptosis through its ability to promote a G1 cell cycle arrest.
26544513 Data show that Ba/F3 cells transformed with mutant HRAS protien indicated equal sensitivity towards Map kinase kinase (MEK) and mTOR serine-threonine kinase (mTOR) inhibition.
26426381 NOTCH1, TP53, and MAP2K1 mutations in splenic diffuse red pulp small B-cell lymphoma are associated with progressive disease.
26384399 Our data demonstrate that MEK inhibitors can inhibit breast cancer stem cells and may have clinical potential for the prevention of metastasis in certain cases in which tumors are MAPK dependent.
26358373 Data show that src kinases (SRC) and mitogen-activated protein kinase kinase 1 (MEK) co-inhibition by saracatinib and PD0325901 respectively can be broadly effective in tumor growth control of a wide panel of non-small cell lung cancer (NSCLC) cell lines.
26324360 MEK1 Mutations are associated with Low-grade Serous Ovarian Cancer.
26208478 Findings suggest that triple therapy directed against BRAF/MEK/ErbB3 may be able to provide durable control of BRAF mutated metastatic melanoma.
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AA Sequence

MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKVGELKDDDFEK      1 - 70
ISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEIS     71 - 140
ICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYLREKHKIMHRDVKPSNILVNSRGEIKLCDFG    141 - 210
VSGQLIDSMANSFVGTRSYMSPERLQGTHYSVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVE    211 - 280
GDAAETPPRPRTPGRPLSSYGMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERA    281 - 350
DLKQLMVHAFIKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV                               351 - 393
//

Text Mined References (312)

PMID Year Title
27098723 2016 ERK1/2, MEK1/2 and p38 downstream signalling molecules impaired in CD56 dim CD16+ and CD56 bright CD16 dim/- natural killer cells in Chronic Fatigue Syndrome/Myalgic Encephalomyelitis patients.
26858456 2016 Endocytosis separates EGF receptors from endogenous fluorescently labeled HRas and diminishes receptor signaling to MAP kinases in endosomes.
26825960 2016 MAPK and SHH pathways modulate type 3 deiodinase expression in papillary thyroid carcinoma.
26625317 2016 Synergistic cooperation between ABT-263 and MEK1/2 inhibitor: effect on apoptosis and proliferation of acute myeloid leukemia cells.
26544513 2015 Mutant HRAS as novel target for MEK and mTOR inhibitors.
26496610 2015 A human interactome in three quantitative dimensions organized by stoichiometries and abundances.
26426381 2016 NOTCH1, TP53, and MAP2K1 Mutations in Splenic Diffuse Red Pulp Small B-cell Lymphoma Are Associated With Progressive Disease.
26384399 2015 MEK Inhibitor Selumetinib (AZD6244; ARRY-142886) Prevents Lung Metastasis in a Triple-Negative Breast Cancer Xenograft Model.
26358373 2015 Combinatorial treatment using targeted MEK and SRC inhibitors synergistically abrogates tumor cell growth and induces mesenchymal-epithelial transition in non-small-cell lung carcinoma.
26324360 2015 Extreme Outlier Analysis Identifies Occult Mitogen-Activated Protein Kinase Pathway Mutations in Patients With Low-Grade Serous Ovarian Cancer.
More...