Page last updated: 2024-08-07 23:48:07

Mitogen-activated protein kinase kinase kinase 12

A mitogen-activated protein kinase kinase kinase 12 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q12852]

Synonyms

EC 2.7.11.25;
Dual leucine zipper bearing kinase;
DLK;
Leucine-zipper protein kinase;
ZPK;
MAPK-upstream kinase;
MUK;
Mixed lineage kinase

Research

Bioassay Publications (3)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's3 (100.00)24.3611
2020's0 (0.00)2.80

Compounds (69)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
staurosporineHomo sapiens (human)IC500.099222

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
imatinibHomo sapiens (human)Kd10.000011
staurosporineHomo sapiens (human)Kd1.500011
gefitinibHomo sapiens (human)Kd10.000011
lestaurtinibHomo sapiens (human)Kd0.840011
vatalanibHomo sapiens (human)Kd10.000011
ruboxistaurinHomo sapiens (human)Kd10.000011
canertinibHomo sapiens (human)Kd10.000011
birb 796Homo sapiens (human)Kd10.000011
sb 203580Homo sapiens (human)Kd10.000011
enzastaurinHomo sapiens (human)Kd10.000011
erlotinibHomo sapiens (human)Kd10.000011
lapatinibHomo sapiens (human)Kd10.000011
sorafenibHomo sapiens (human)Kd10.000011
pd 173955Homo sapiens (human)Kd10.000011
s 1033Homo sapiens (human)Kd10.000011
bms 387032Homo sapiens (human)Kd10.000011
tandutinibHomo sapiens (human)Kd10.000011
vx-745Homo sapiens (human)Kd10.000011
dasatinibHomo sapiens (human)Kd10.000011
zd 6474Homo sapiens (human)Kd10.000011
alvocidibHomo sapiens (human)Kd10.000011
bosutinibHomo sapiens (human)Kd0.670011
su 11248Homo sapiens (human)Kd0.100011
vx680Homo sapiens (human)Kd0.190011
axitinibHomo sapiens (human)Kd1.700011
pd 184352Homo sapiens (human)Kd10.000011
bms345541Homo sapiens (human)Kd10.000011
midostaurinHomo sapiens (human)Kd10.000011
ki 20227Homo sapiens (human)Kd10.000011
pi103Homo sapiens (human)Kd10.000011
hki 272Homo sapiens (human)Kd0.370011
tofacitinibHomo sapiens (human)Kd10.000011
n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamideHomo sapiens (human)Kd10.000011
cediranibHomo sapiens (human)Kd10.000011
masitinibHomo sapiens (human)Kd10.000011
pazopanibHomo sapiens (human)Kd10.000011
azd 6244Homo sapiens (human)Kd10.000011
su 14813Homo sapiens (human)Kd0.560011
bibw 2992Homo sapiens (human)Kd10.000011
tg100-115Homo sapiens (human)Kd10.000011
pha 665752Homo sapiens (human)Kd0.670011
6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-oneHomo sapiens (human)Kd10.000011
brivanibHomo sapiens (human)Kd10.000011
at 7519Homo sapiens (human)Kd10.000011
bi 2536Homo sapiens (human)Kd10.000011
nvp-ast487Homo sapiens (human)Kd2.500011
kw 2449Homo sapiens (human)Kd0.067011
abt 869Homo sapiens (human)Kd10.000011
gw 2580Homo sapiens (human)Kd10.000011
crizotinibHomo sapiens (human)Kd0.170011
chir-265Homo sapiens (human)Kd10.000011
motesanibHomo sapiens (human)Kd10.000011
mln8054Homo sapiens (human)Kd10.000011
GDC-0879Homo sapiens (human)Kd10.000011
gsk 461364Homo sapiens (human)Kd10.000011
azd 1152-hqpaHomo sapiens (human)Kd10.000011
nvp-tae684Homo sapiens (human)Kd0.042011
fedratinibHomo sapiens (human)Kd6.300011
gsk690693Homo sapiens (human)Kd10.000011
gdc 0941Homo sapiens (human)Kd10.000011
plx 4720Homo sapiens (human)Kd10.000011
sgx 523Homo sapiens (human)Kd10.000011
quizartinibHomo sapiens (human)Kd10.000011
incb-018424Homo sapiens (human)Kd10.000011
gsk 1838705aHomo sapiens (human)Kd10.000011
gsk 1363089Homo sapiens (human)Kd0.022011
chir 258Homo sapiens (human)Kd2.100011
nintedanibHomo sapiens (human)Kd0.140011
pp242Homo sapiens (human)Kd10.000011

Enables

This protein enables 9 target(s):

TargetCategoryDefinition
protein kinase activitymolecular functionCatalysis of the phosphorylation of an amino acid residue in a protein, usually according to the reaction: a protein + ATP = a phosphoprotein + ADP. [PMID:25399640]
protein serine/threonine kinase activitymolecular functionCatalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:bf, MetaCyc:PROTEIN-KINASE-RXN, PMID:2956925]
protein bindingmolecular functionBinding to a protein. [GOC:go_curators]
ATP bindingmolecular functionBinding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732]
protein kinase bindingmolecular functionBinding to a protein kinase, any enzyme that catalyzes the transfer of a phosphate group, usually from ATP, to a protein substrate. [GOC:jl]
protein homodimerization activitymolecular functionBinding to an identical protein to form a homodimer. [GOC:jl]
protein serine/threonine kinase activator activitymolecular functionBinds to and increases the activity of a protein serine/threonine kinase. [GOC:go_curators]
protein serine kinase activitymolecular functionCatalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989]
JUN kinase kinase kinase activitymolecular functionCatalysis of the reaction: JNKK + ATP = JNKK phosphate + ADP. This reaction is the phosphorylation and activation of JUN kinase kinases (JNKKs). [GOC:bf]

Located In

This protein is located in 5 target(s):

TargetCategoryDefinition
cytoplasmcellular componentThe contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684]
cytosolcellular componentThe part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl]
plasma membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]
membranecellular componentA lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194]
growth conecellular componentThe migrating motile tip of a growing neuron projection, where actin accumulates, and the actin cytoskeleton is the most dynamic. [GOC:aruk, GOC:bc, ISBN:0815316194, PMID:10082468]

Involved In

This protein is involved in 11 target(s):

TargetCategoryDefinition
protein phosphorylationbiological processThe process of introducing a phosphate group on to a protein. [GOC:hb]
JNK cascadebiological processA MAPK cascade containing at least the JNK (MAPK8) MAP kinase. It starts with the activation of JUN3K (a MAPK3K), which activates JNKK a MAP2K), which in turn activates JNK. The cascade can also contain an additional tier: the upstream MAP4K. The kinases in each tier phosphorylate and activate the kinases in the downstream tier. The JNK cascade is activated by stress signals, as well as by G protein-coupled receptors, growth factors, and cytokines, and results in cellular responses such as cell proliferation, cell differentiation, apoptosis and inflammation. [PMID:11790549, PMID:20811974, PMID:23125017]
peptidyl-serine phosphorylationbiological processThe phosphorylation of peptidyl-serine to form peptidyl-O-phospho-L-serine. [RESID:AA0037]
intracellular signal transductionbiological processThe process in which a signal is passed on to downstream components within the cell, which become activated themselves to further propagate the signal and finally trigger a change in the function or state of the cell. [GOC:bf, GOC:jl, GOC:signaling, ISBN:3527303782]
positive regulation of JUN kinase activitybiological processAny process that activates or increases the frequency, rate or extent of JUN kinase activity. [GOC:jl]
post-translational protein modificationbiological processThe process of covalently altering one or more amino acids in a protein after the protein has been completely translated and released from the ribosome. [GOC:jsg]
positive regulation of protein kinase activitybiological processAny process that activates or increases the frequency, rate or extent of protein kinase activity. [GOC:go_curators]
positive regulation of DNA-templated transcriptionbiological processAny process that activates or increases the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH]
protein autophosphorylationbiological processThe phosphorylation by a protein of one or more of its own amino acid residues (cis-autophosphorylation), or residues on an identical protein (trans-autophosphorylation). [ISBN:0198506732]
positive regulation of ERK1 and ERK2 cascadebiological processAny process that activates or increases the frequency, rate or extent of signal transduction mediated by the ERK1 and ERK2 cascade. [GOC:mah]
negative regulation of motor neuron apoptotic processbiological processAny process that stops, prevents or reduces the frequency, rate or extent of motor neuron apoptotic process. [GOC:mtg_apoptosis, GOC:obol]