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mitogen-activated protein kinase kinase kinase 1

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Target not currently curated in GtoImmuPdb

Target id: 2069

Nomenclature: mitogen-activated protein kinase kinase kinase 1

Abbreviated Name: MEKK1

Family: STE11 family

Contents:

Gene and Protein Information Click here for help
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 63.36 cM Map3k1 mitogen-activated protein kinase kinase kinase 1
Rat - 1493 2q14 Map3k1 mitogen-activated protein kinase kinase kinase 1
Previous and Unofficial Names Click here for help
MAPK/ERK kinase kinase 1 | MAPKKK1 | MEK kinase 1 | mitogen-activated protein kinase kinase kinase 1, E3 ubiquitin protein ligase
Database Links Click here for help
Alphafold Q13233 (Hs), P53349 (Mm), Q62925 (Rn)
BRENDA 2.7.11.25
CATH/Gene3D 3.30.40.10
ChEMBL Target CHEMBL3956 (Hs)
Ensembl Gene ENSG00000095015 (Hs), ENSMUSG00000021754 (Mm), ENSRNOG00000013177 (Rn)
Entrez Gene 4214 (Hs), 26401 (Mm), 116667 (Rn)
Human Protein Atlas ENSG00000095015 (Hs)
KEGG Enzyme 2.7.11.25
KEGG Gene hsa:4214 (Hs), mmu:26401 (Mm), rno:116667 (Rn)
OMIM 600982 (Hs)
Orphanet ORPHA260583 (Hs)
Pharos Q13233 (Hs)
RefSeq Nucleotide NM_005921 (Hs), NM_011945 (Mm), NM_053887 (Rn)
RefSeq Protein NP_005912 (Hs), NP_036075 (Mm), NP_446339 (Rn)
UniProtKB Q13233 (Hs), P53349 (Mm), Q62925 (Rn)
Wikipedia MAP3K1 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.25

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
E6201 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.5 pIC50 2
⤷ pIC50 7.5 (IC50 3.1x10-8 M) [2]
DiscoveRx KINOMEscan® screen Click here for help
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.0 pKd
GSK-461364A Small molecule or natural product Hs Inhibitor Inhibition 5.8 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 5.7 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.6 pKd
pazopanib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 5.5 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Immune regulation
Immuno Process:  Cellular signalling
Clinically-Relevant Mutations and Pathophysiology Click here for help
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 08/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2069.