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TAO kinase 2

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Target not currently curated in GtoImmuPdb

Target id: 2234

Nomenclature: TAO kinase 2

Abbreviated Name: TAO2

Family: TAO subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 5 1235 16p11.2 TAOK2 TAO kinase 2
Mouse 5 1240 7 F3 Taok2 TAO kinase 2
Rat 5 1235 1q36-q37 Taok2 TAO kinase 2
Previous and Unofficial Names Click here for help
MAP3K17 | PSK1 | thousand and one amino acid protein 2
Database Links Click here for help
Alphafold Q9UL54 (Hs), Q6ZQ29 (Mm), Q9JLS3 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL1075195 (Hs), CHEMBL4523465 (Rn)
Ensembl Gene ENSG00000149930 (Hs), ENSMUSG00000059981 (Mm), ENSRNOG00000019964 (Rn)
Entrez Gene 9344 (Hs), 381921 (Mm), 64666 (Rn)
Human Protein Atlas ENSG00000149930 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:9344 (Hs), mmu:381921 (Mm), rno:64666 (Rn)
OMIM 613199 (Hs)
Pharos Q9UL54 (Hs)
RefSeq Nucleotide NM_001252043 (Hs), NM_001163774 (Mm), NM_022702 (Rn)
RefSeq Protein NP_004774 (Hs), NP_001157246 (Mm), NP_073193 (Rn)
UniProtKB Q9UL54 (Hs), Q6ZQ29 (Mm), Q9JLS3 (Rn)
Wikipedia TAOK2 (Hs)
Selected 3D Structures Click here for help
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:  6
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:  7
Enzyme Reaction Click here for help
EC Number: 2.7.11.1

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
AMG28 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.0 pIC50 3
⤷ pIC50 7.0 (IC50 9.1x10-8 M) [3]
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: 2,5
Key to terms and symbols Click column headers to sort
Target used in screen: TAOK2
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 7.4 pKd
AT-7519 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
CHIR-265 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
alvocidib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.5 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand 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 Click here for help
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: 1,4
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 1.0 0.5 -0.5
JNJ-7706621 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.9 6.0 2.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 11.5 2.0 3.0
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 13.3 10.0 9.0
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 18.6
SU11274 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 21.9 19.0 4.0
pazopanib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 26.8
sorafenib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 36.9
K-252a Small molecule or natural product Hs Inhibitor Inhibition 40.5 16.0 2.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure 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. Drewry DH, Potjewyd FM, Bayati A, Smith JL, Dickmander RJ, Howell S, Taft-Benz S, Min SM, Hossain MA, Heise M et al.. (2022) Identification and Utilization of a Chemical Probe to Interrogate the Roles of PIKfyve in the Lifecycle of β-Coronaviruses. J Med Chem, 65 (19): 12860-12882. [PMID:36111834]

4. 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]

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]

6. 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]

7. 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 20/09/2022. Accessed on 18/01/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2234.