TAO kinase 2 | TAO subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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TAO kinase 2

Target not currently curated in GtoImmuPdb

Target id: 2234

Nomenclature: TAO kinase 2

Abbreviated Name: TAO2

Family: TAO subfamily

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 - 1049 16p11.2 TAOK2 TAO kinase 2
Mouse - 1055 7 F3 Taok2 TAO kinase 2
Rat - 1235 1 q36 Taok2 TAO kinase 2
Previous and Unofficial Names
MAP3K17 | PSK1 | thousand and one amino acid protein 2
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the TAO2 kinase domain: activation and specifity of a Ste20p MAP3K.
PDB Id:  1U5Q
Resolution:  2.1Å
Species:  Rat
References:  5
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the MAP3K TAO2 kinase domain bound by an inhibitor staurosporine.
PDB Id:  2GCD
Ligand:  staurosporine
Resolution:  2.55Å
Species:  Rat
References:  6
Enzyme Reaction
EC Number: 2.7.11.1
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: 2,4

Key to terms and symbols Click column headers to sort
Target used in screen: TAOK2
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 7.9 pKd
AST-487 Hs Inhibitor Inhibition 7.4 pKd
AT-7519 Hs Inhibitor Inhibition 7.3 pKd
CHIR-265 Hs Inhibitor Inhibition 6.8 pKd
alvocidib Hs Inhibitor Inhibition 6.6 pKd
ruxolitinib Hs Inhibitor Inhibition 6.5 pKd
PP-242 Hs Inhibitor Inhibition 6.4 pKd
tozasertib Hs Inhibitor Inhibition 6.4 pKd
PD-173955 Hs Inhibitor Inhibition 6.4 pKd
lestaurtinib Hs Inhibitor Inhibition 6.3 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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: TAO2/TAOK2(TAO1)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 1.0 0.5 -0.5
JNJ-7706621 Hs Inhibitor Inhibition 8.9 6.0 2.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 11.5 2.0 3.0
Gö 6976 Hs Inhibitor Inhibition 13.3 10.0 9.0
tozasertib Hs Inhibitor Inhibition 18.6
SU11274 Hs Inhibitor Inhibition 21.9 19.0 4.0
pazopanib Hs Inhibitor Inhibition 26.8
sorafenib Hs Inhibitor Inhibition 36.9
K-252a Hs Inhibitor Inhibition 40.5 16.0 2.0
PKR inhibitor Hs Inhibitor Inhibition 56.9 33.0 10.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1039-45. [PMID:22037377]

2. 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]

3. 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]

4. 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]

5. Zhou T, Raman M, Gao Y, Earnest S, Chen Z, Machius M, Cobb MH, Goldsmith EJ. (2004) Crystal structure of the TAO2 kinase domain: activation and specificity of a Ste20p MAP3K. Structure, 12 (10): 1891-900. [PMID:15458637]

6. Zhou TJ, Sun LG, Gao Y, Goldsmith EJ. (2006) Crystal structure of the MAP3K TAO2 kinase domain bound by an inhibitor staurosporine. Acta Biochim. Biophys. Sin. (Shanghai), 38 (6): 385-92. [PMID:16761096]

How to cite this page

TAO subfamily: TAO kinase 2. Last modified on 27/03/2013. Accessed on 05/12/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2234.