mitogen-activated protein kinase kinase 7 | STE7 family | IUPHAR/BPS Guide to PHARMACOLOGY

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mitogen-activated protein kinase kinase 7

Target not currently curated in GtoImmuPdb

Target id: 2068

Nomenclature: mitogen-activated protein kinase kinase 7

Abbreviated Name: MKK7

Family: STE7 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 - 419 19p13.3-p13.2 MAP2K7 mitogen-activated protein kinase kinase 7
Mouse - 419 8 A1.1 Map2k7 mitogen-activated protein kinase kinase 7
Rat - 419 12 p12 Map2k7 mitogen activated protein kinase kinase 7
Gene and Protein Information Comments
Multiple alternatively spliced transcript variants encoding distinct isoforms have been found, but only the transcript variant generating the 419 amino acid protein has been supported and defined. Isoform B is postulated to contain a 43 amino acid insertion, translating to a 462 amino acid protein.
Previous and Unofficial Names
PRKMK7 | c-Jun N-terminal kinase kinase 2 | dual specificity mitogen-activated protein kinase kinase 7 | JNK kinase 2 | JNKK2 | MAP kinase kinase 7 | MKK7 | SAPKK4 | sek2 | SKK4 | Stress-activated protein kinase kinase 4
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.12.2

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 Affinity Parameter Reference
compound 11 [PMID: 26431428] Hs Inhibition 5.3 pIC50 3
pIC50 5.3 (IC50 5x10-6 M) [3]
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Parameter Reference
cobimetinib Hs Negative <5.0 pIC50 4
pIC50 <5.0 (IC50 >1x10-5 M) [4]
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: 1,5

Key to terms and symbols Click column headers to sort
Target used in screen: MKK7
Ligand Sp. Type Action Affinity Parameter
AST-487 Hs Inhibitor Inhibition 7.6 pKd
staurosporine Hs Inhibitor Inhibition 7.5 pKd
lestaurtinib Hs Inhibitor Inhibition 7.1 pKd
canertinib Hs Inhibitor Inhibition 7.0 pKd
neratinib Hs Inhibitor Inhibition 6.3 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
erlotinib 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 »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: 2...

Key to terms and symbols Click column headers to sort
Target used in screen: MKK7β/nd
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Hs Inhibitor Inhibition 7.0 0.0
JNK inhibitor VIII Hs Inhibitor Inhibition 11.0 4.0
staurosporine Hs Inhibitor Inhibition 11.0 1.5
isogranulatimide Hs Inhibitor Inhibition 42.0 27.0
PKR inhibitor Hs Inhibitor Inhibition 43.0 12.0
Gö 6976 Hs Inhibitor Inhibition 52.0 34.0
indirubin-3'-monoxime Hs Inhibitor Inhibition 52.0 7.0
indirubin derivative E804 Hs Inhibitor Inhibition 54.0 5.0
Cdk2 inhibitor IV Hs Inhibitor Inhibition 56.0 16.0
SP600125 Hs Inhibitor Inhibition 58.0 6.0
Displaying the top 10 most potent ligands  View all ligands in screen »

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. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J., 451 (2): 313-28. [PMID:23398362]

3. Patel S, Harris SF, Gibbons P, Deshmukh G, Gustafson A, Kellar T, Lin H, Liu X, Liu Y, Liu Y et al.. (2015) Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12). J. Med. Chem., 58 (20): 8182-99. [PMID:26431428]

4. Rice KD, Aay N, Anand NK, Blazey CM, Bowles OJ, Bussenius J, Costanzo S, Curtis JK, Defina SC, Dubenko L et al.. (2012) Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973). ACS Med. Che. Letters, 3 (5): 416–421.

5. 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

STE7 family: mitogen-activated protein kinase kinase 7. Last modified on 19/06/2018. Accessed on 23/05/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2068.