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)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 3 (100.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (69)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| staurosporine | Homo sapiens (human) | IC50 | 0.0992 | 2 | 2 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| imatinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | Kd | 1.5000 | 1 | 1 |
| gefitinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| lestaurtinib | Homo sapiens (human) | Kd | 0.8400 | 1 | 1 |
| vatalanib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| ruboxistaurin | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| canertinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| birb 796 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| sb 203580 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| enzastaurin | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| erlotinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| lapatinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| sorafenib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pd 173955 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| s 1033 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| bms 387032 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| tandutinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| vx-745 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| dasatinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| zd 6474 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| alvocidib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| bosutinib | Homo sapiens (human) | Kd | 0.6700 | 1 | 1 |
| su 11248 | Homo sapiens (human) | Kd | 0.1000 | 1 | 1 |
| vx680 | Homo sapiens (human) | Kd | 0.1900 | 1 | 1 |
| axitinib | Homo sapiens (human) | Kd | 1.7000 | 1 | 1 |
| pd 184352 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| bms345541 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| midostaurin | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| ki 20227 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pi103 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| hki 272 | Homo sapiens (human) | Kd | 0.3700 | 1 | 1 |
| tofacitinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamide | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| cediranib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| masitinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pazopanib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| azd 6244 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| su 14813 | Homo sapiens (human) | Kd | 0.5600 | 1 | 1 |
| bibw 2992 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| tg100-115 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pha 665752 | Homo sapiens (human) | Kd | 0.6700 | 1 | 1 |
| 6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| brivanib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| at 7519 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| bi 2536 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| nvp-ast487 | Homo sapiens (human) | Kd | 2.5000 | 1 | 1 |
| kw 2449 | Homo sapiens (human) | Kd | 0.0670 | 1 | 1 |
| abt 869 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gw 2580 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| crizotinib | Homo sapiens (human) | Kd | 0.1700 | 1 | 1 |
| chir-265 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| motesanib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| mln8054 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| GDC-0879 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gsk 461364 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| azd 1152-hqpa | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| nvp-tae684 | Homo sapiens (human) | Kd | 0.0420 | 1 | 1 |
| fedratinib | Homo sapiens (human) | Kd | 6.3000 | 1 | 1 |
| gsk690693 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gdc 0941 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| plx 4720 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| sgx 523 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| quizartinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| incb-018424 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gsk 1838705a | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gsk 1363089 | Homo sapiens (human) | Kd | 0.0220 | 1 | 1 |
| chir 258 | Homo sapiens (human) | Kd | 2.1000 | 1 | 1 |
| nintedanib | Homo sapiens (human) | Kd | 0.1400 | 1 | 1 |
| pp242 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
Enables
This protein enables 9 target(s):
| Target | Category | Definition |
|---|---|---|
| protein kinase activity | molecular function | Catalysis 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 activity | molecular function | Catalysis 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 binding | molecular function | Binding to a protein. [GOC:go_curators] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| protein kinase binding | molecular function | Binding 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 activity | molecular function | Binding to an identical protein to form a homodimer. [GOC:jl] |
| protein serine/threonine kinase activator activity | molecular function | Binds to and increases the activity of a protein serine/threonine kinase. [GOC:go_curators] |
| protein serine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989] |
| JUN kinase kinase kinase activity | molecular function | Catalysis 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):
| Target | Category | Definition |
|---|---|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| cytosol | cellular component | The 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 membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| growth cone | cellular component | The 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):
| Target | Category | Definition |
|---|---|---|
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| JNK cascade | biological process | A 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 phosphorylation | biological process | The phosphorylation of peptidyl-serine to form peptidyl-O-phospho-L-serine. [RESID:AA0037] |
| intracellular signal transduction | biological process | The 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 activity | biological process | Any process that activates or increases the frequency, rate or extent of JUN kinase activity. [GOC:jl] |
| post-translational protein modification | biological process | The 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 activity | biological process | Any process that activates or increases the frequency, rate or extent of protein kinase activity. [GOC:go_curators] |
| positive regulation of DNA-templated transcription | biological process | Any process that activates or increases the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
| protein autophosphorylation | biological process | The 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 cascade | biological process | Any 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 process | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of motor neuron apoptotic process. [GOC:mtg_apoptosis, GOC:obol] |