Page last updated: 2024-08-07 13:16:55

Mitogen-activated protein kinase kinase kinase 8

A mitogen-activated protein kinase kinase kinase 8 that is encoded in the genome of human. [PRO:DNx]

Synonyms

EC 2.7.11.25;
Cancer Osaka thyroid oncogene;
Proto-oncogene c-Cot;
Serine/threonine-protein kinase cot;
Tumor progression locus 2;
TPL-2

Research

Bioassay Publications (9)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (44.44)29.6817
2010's5 (55.56)24.3611
2020's0 (0.00)2.80

Compounds (10)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
ro 31-8220Homo sapiens (human)IC509.950011
gefitinibHomo sapiens (human)IC501.000011
ellagic acidHomo sapiens (human)IC502.370011
a 770041Homo sapiens (human)IC5025.000011
pd 0325901Homo sapiens (human)IC5025.000011
nvp-aew541Homo sapiens (human)IC5010.000011
pf 00299804Homo sapiens (human)IC503.570011
4-[2-(2-chloro-4-fluoroanilino)-5-methyl-4-pyrimidinyl]-N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamideHomo sapiens (human)Ki4.000011
2-({2-[(3-hydroxyphenyl)amino]pyrimidin-4-yl}amino)benzamideHomo sapiens (human)IC5050.000011
8-chloro-4-(3-chloro-4-fluoroanilino)-6-[[1-(1-ethyl-4-piperidinyl)-4-triazolyl]methylamino]-3-quinolinecarbonitrileHomo sapiens (human)IC500.001622

Enables

This protein enables 6 target(s):

TargetCategoryDefinition
magnesium ion bindingmolecular functionBinding to a magnesium (Mg) ion. [GOC:ai]
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]
MAP kinase kinase kinase activitymolecular functionCatalysis of the phosphorylation and activation of a MAP kinase kinase; each MAP kinase kinase can be phosphorylated by any of several MAP kinase kinase kinases. [PMID:9561267]
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 serine kinase activitymolecular functionCatalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989]

Located In

This protein is located in 1 target(s):

TargetCategoryDefinition
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]

Involved In

This protein is involved in 3 target(s):

TargetCategoryDefinition
MAPK cascadebiological processAn intracellular protein kinase cascade containing at least a MAP kinase (MAPK). It starts with the activation of a MAP3K, and the consecutive activation of a MPK2K and a MAPK. The cascade can also contain an additional tier: the upstream MAP4K. The kinases in each tier phosphorylate and activate the kinase in the downstream tier to transmit a signal within a cell. [PMID:20811974, PMID:9561267]
protein phosphorylationbiological processThe process of introducing a phosphate group on to a protein. [GOC:hb]
T cell costimulationbiological processThe process of providing, via surface-bound receptor-ligand pairs, a second, antigen-independent, signal in addition to that provided by the T cell receptor to augment T cell activation. [ISBN:0781735149]