Property Summary

NCBI Gene PubMed Count 60
Grant Count 64
R01 Count 44
Funding $2,873,364.66
PubMed Score 53.03
PubTator Score 47.67

Knowledge Summary

Patent (7,681)

TINX Plot

Expression

  Differential Expression (3)

Disease log2 FC p
osteosarcoma -1.968 0.000
non-small cell lung cancer -1.190 0.000
ovarian cancer -1.800 0.000

Synonym

Accession Q99759 B2RCW2 D3DU15 Q5BKZ6 Q8N3I9
Symbols MEKK3
MAPKKK3

Gene

PDB

4Y5O   4YL6   2C60   2JRH   2O2V   2PPH  

  TechDev Info (1)

Gary Johnson Kinome profile via MIB/MS Technology

 GWAS Trait (1)

MLP Assay (6)

AID Type Active / Inconclusive / Inactive Description
1529 screening 4159 / 151 / 285664 Multiplex HTS Assay for Inhibitors of MEK Kinase PB1 Domains, specifically MEK5 MEK Kinase3 Wildtype
1894 screening 105 / 0 / 5837 Single Concentration Confirmation Screen via Multiplex HTS Assay for Inhibitors of MEK Kinase PB1 Domains, specifically MEK5 MEK Kinase3 Wildtype
1896 confirmatory 33 / 0 / 153 Dose Response Confirmation Screen via Multiplex HTS Assay for Inhibitors of MEK Kinase PB1 Domains, specifically MEK5 binding to MEK Kinase 3 Wildtype
1982 other 0 / 0 / 0 Kinase inhibition selectivity assay for compound SID-48409448
2145 confirmatory 0 / 0 / 13 SAR Compounds tested by Dose Response Screen via Multiplex HTS Assay for Inhibitors of MEK Kinase PB1 Domains, specifically MEK5 binding to MEK Kinase 3 Wildtype.
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 (32)

PMID Text
27027284 studies identify gain of MEKK3 signalling and KLF2/4 function as causal mechanisms for cerebral cavernous malformations pathogenesis that may be targeted to develop new CCM therapeutics
26997451 MAP3K3 overexpression is an independent poor prognostic indicator in ovarian carcinoma.
26304632 Polymorphisms in MAP3K3, MMP24 and IGF1R are associated with greater height and act additively on height in children of an admixed population.
26088427 MAP3K3 may potentially not only serve as diagnostic/prognostic markers for patients with lung cancer but also provide an indicator for future investigations into immunomodulatory therapies for lung cancer.
25824786 High MEKK3 expression is associated with renal clear cell carcinoma.
25728774 Our finding that Verrucous venous malformation contains a MAP3K3 mutation supports our impression that this lesion is a venous anomaly.
25388155 MEKK3 expression was significantly higher in patients with renal clear cell carcinoma than in controls.
25043814 This study identified an NBR1-MEKK3 complex as a key regulator of JNK signaling and adipose tissue inflammation in obesity.
25040987 MEKK3 expression was positively correlated with survivin.
24975362 Inhibitors of apoptosis proteins regulate myogenic differentiation by directly suppressing MEKK2/3-MEK5-ERK5 signaling.
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AA Sequence

MDEQEALNSIMNDLVALQMNRRHRMPGYETMKNKDTGHSNRQSDVRIKFEHNGERRIIAFSRPVKYEDVE      1 - 70
HKVTTVFGQPLDLHYMNNELSILLKNQDDLDKAIDILDRSSSMKSLRILLLSQDRNHNSSSPHSGVSRQV     71 - 140
RIKASQSAGDINTIYQPPEPRSRHLSVSSQNPGRSSPPPGYVPERQQHIARQGSYTSINSEGEFIPETSE    141 - 210
QCMLDPLSSAENSLSGSCQSLDRSADSPSFRKSRMSRAQSFPDNRQEYSDRETQLYDKGVKGGTYPRRYH    211 - 280
VSVHHKDYSDGRRTFPRIRRHQGNLFTLVPSSRSLSTNGENMGLAVQYLDPRGRLRSADSENALSVQERN    281 - 350
VPTKSPSAPINWRRGKLLGQGAFGRVYLCYDVDTGRELASKQVQFDPDSPETSKEVSALECEIQLLKNLQ    351 - 420
HERIVQYYGCLRDRAEKTLTIFMEYMPGGSVKDQLKAYGALTESVTRKYTRQILEGMSYLHSNMIVHRDI    421 - 490
KGANILRDSAGNVKLGDFGASKRLQTICMSGTGMRSVTGTPYWMSPEVISGEGYGRKADVWSLGCTVVEM    491 - 560
LTEKPPWAEYEAMAAIFKIATQPTNPQLPSHISEHGRDFLRRIFVEARQRPSAEELLTHHFAQLMY        561 - 626
//

Text Mined References (69)

PMID Year Title
27027284 2016 Cerebral cavernous malformations arise from endothelial gain of MEKK3-KLF2/4 signalling.
26997451 2016 MAP3K3 overexpression is associated with poor survival in ovarian carcinoma.
26304632 2015 Association Study of GWAS-Derived Loci with Height in Brazilian Children: Importance of MAP3K3, MMP24 and IGF1R Polymorphisms for Height Variation.
26088427 2015 MAP3K3 expression in tumor cells and tumor-infiltrating lymphocytes is correlated with favorable patient survival in lung cancer.
25824786 2015 Expression and prognostic role of MEKK3 and pERK in patients with renal clear cell carcinoma.
25728774 2015 A somatic MAP3K3 mutation is associated with verrucous venous malformation.
25429064 2015 Meta-analysis of genome-wide association studies of adult height in East Asians identifies 17 novel loci.
25388155 2015 The expression and role of MEKK3 in renal clear cell carcinoma.
25241761 2014 Using an in situ proximity ligation assay to systematically profile endogenous protein-protein interactions in a pathway network.
25043814 2014 A macrophage NBR1-MEKK3 complex triggers JNK-mediated adipose tissue inflammation in obesity.
More...