mitogen-activated protein kinase kinase kinase 1 | STE11 family | IUPHAR/BPS Guide to PHARMACOLOGY

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mitogen-activated protein kinase kinase kinase 1

Target not currently curated in GtoImmuPdb

Target id: 2069

Nomenclature: mitogen-activated protein kinase kinase kinase 1

Abbreviated Name: MEKK1

Family: STE11 family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1512 5q11.2 MAP3K1 mitogen-activated protein kinase kinase kinase 1
Mouse - 1493 13 D2.2 Map3k1 mitogen-activated protein kinase kinase kinase 1
Rat - 1493 2 q14 Map3k1 mitogen-activated protein kinase kinase kinase 1
Previous and Unofficial Names
MAPK/ERK kinase kinase 1 | MAPKKK1 | MEK kinase 1 | mitogen-activated protein kinase kinase kinase 1, E3 ubiquitin protein ligase
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.11.25

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
E6201 Hs Inhibition 7.5 pIC50 2
pIC50 7.5 (IC50 3.1x10-8 M) [2]
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: MAP3K1
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 6.5 pKd
crizotinib Hs Inhibitor Inhibition 6.0 pKd
GSK-461364A Hs Inhibitor Inhibition 5.8 pKd
AST-487 Hs Inhibitor Inhibition 5.7 pKd
PP-242 Hs Inhibitor Inhibition 5.6 pKd
pazopanib Hs Inhibitor Inhibition 5.5 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Hs Inhibitor Inhibition <5.5 pKd
masitinib Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes
GO:0002755 MyD88-dependent toll-like receptor signaling pathway TAS
Immuno Process:  Immune regulation
GO Annotations:  Associated to 2 GO processes
GO:0002755 MyD88-dependent toll-like receptor signaling pathway TAS
GO:0038095 Fc-epsilon receptor signaling pathway TAS
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 4 GO processes
GO:0000209 protein polyubiquitination IMP
GO:0002755 MyD88-dependent toll-like receptor signaling pathway TAS
GO:0004842 ubiquitin-protein transferase activity ISO
GO:0038095 Fc-epsilon receptor signaling pathway TAS
Clinically-Relevant Mutations and Pathophysiology
Disease:  46, XY sex reversal 6; SRXY6
Synonyms: 46,XY complete gonadal dysgenesis [Orphanet: ORPHA242]
46 XY gonadal dysgenesis [Disease Ontology: DOID:14448]
46,XY partial gonadal dysgenesis [Orphanet: ORPHA251510]
Disease Ontology: DOID:14448
OMIM: 613762
Orphanet: ORPHA242, ORPHA251510

References

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1. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1046-51. [PMID:22037378]

2. Goto M, Chow J, Muramoto K, Chiba K, Yamamoto S, Fujita M, Obaishi H, Tai K, Mizui Y, Tanaka I et al.. (2009) E6201 [(3S,4R,5Z,8S,9S,11E)-14-(ethylamino)-8, 9,16-trihydroxy-3,4-dimethyl-3,4,9,19-tetrahydro-1H-2-benzoxacyclotetradecine-1,7(8H)-dione], a novel kinase inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase (MEK)-1 and MEK kinase-1: in vitro characterization of its anti-inflammatory and antihyperproliferative activities. J. Pharmacol. Exp. Ther., 331 (2): 485-95. [PMID:19684251]

3. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol., 17 (11): 1241-9. [PMID:21095574]

How to cite this page

STE11 family: mitogen-activated protein kinase kinase kinase 1. Last modified on 30/03/2016. Accessed on 05/04/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2069.