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Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 1001 | 17q11.2 | TAOK1 | TAO kinase 1 | |
Mouse | - | 1001 | 11 B5 | Taok1 | TAO kinase 1 | |
Rat | - | 1001 | 10q24 | Taok1 | TAO kinase 1 |
Previous and Unofficial Names |
MAP3K16 | MARKK | prostate-derived sterile 20 (Ste20)-like kinase 2 | PSK2 | thousand and one amino acid protein 1 | thousand and one kinase 1 |
Database Links | |
Alphafold | Q7L7X3 (Hs), Q5F2E8 (Mm), O88664 (Rn) |
BRENDA | 2.7.11.1 |
ChEMBL Target | CHEMBL5261 (Hs) |
Ensembl Gene | ENSG00000160551 (Hs), ENSMUSG00000017291 (Mm), ENSRNOG00000015692 (Rn) |
Entrez Gene | 57551 (Hs), 216965 (Mm), 286993 (Rn) |
Human Protein Atlas | ENSG00000160551 (Hs) |
KEGG Enzyme | 2.7.11.1 |
KEGG Gene | hsa:57551 (Hs), mmu:216965 (Mm), rno:286993 (Rn) |
OMIM | 610266 (Hs) |
Pharos | Q7L7X3 (Hs) |
RefSeq Nucleotide | NM_020791 (Hs), NM_144825 (Mm), NM_173327 (Rn) |
RefSeq Protein | NP_065842 (Hs), NP_659074 (Mm), NP_775449 (Rn) |
UniProtKB | Q7L7X3 (Hs), Q5F2E8 (Mm), O88664 (Rn) |
Wikipedia | TAOK1 (Hs) |
Enzyme Reaction | ||||
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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 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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: 2,8 |
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Target used in screen: TAOK1 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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: 1,5 |
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Target used in screen: TAO1/TAOK1 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Immunopharmacology Comments |
TAOK1 has been discovered to function as a negative regulator of IL-17 (IL-17A)-mediated signal transduction and inflammation [9]. IL-17 is a proinflammatory cytokine involved in the development of several autoimmune diseases, including inflammatory bowel disease and Sjögren's syndrome. TAOK1 appears to interact with IL-17RA, and this action prevents IL-17RA-Act1-TRAF6 signaling complex formation, and inhibits NF-κB and MAP kinase pathway activation. This in turn leads to a reduction in the expression of IL-17-induced proinflammatory mediators (e.g. IL-6, CXCL1, CXCL2, CCL20 and CSF3). TAOK1 is revealed as a component of the regulatory system that controls IL-17activity that is necessary to limit harmful IL-17-driven inflammation and autoimmune disease. Decreased TAOK1 expression has been reported in the colons of ulcerative colitis patients. Thus, the accumulating evidence delineating TAOK1 's functions indicate that this kinase is involved in the pathogenesis of IL-17-related autoimmune conditions. |
Physiological Consequences of Altering Gene Expression | ||||||||||
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General Comments |
As well as being a member of the STE20-like kinases family, TAOK1 is also a member of the MAP kinase kinase kinase family, and is involved in MAPK signaling. It is reported to be involved in microtubule dynamics and mitotic progression [3], and the p38 and JNK response to DNA damage and stress stimuli [7]. |
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. Draviam VM, Stegmeier F, Nalepa G, Sowa ME, Chen J, Liang A, Hannon GJ, Sorger PK, Harper JW, Elledge SJ. (2007) A functional genomic screen identifies a role for TAO1 kinase in spindle-checkpoint signalling. Nat Cell Biol, 9 (5): 556-64. [PMID:17417629]
4. 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]
5. 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]
6. Menichincheri M, Albanese C, Alli C, Ballinari D, Bargiotti A, Caldarelli M, Ciavolella A, Cirla A, Colombo M, Colotta F et al.. (2010) Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding. J Med Chem, 53 (20): 7296-315. [PMID:20873740]
7. Raman M, Earnest S, Zhang K, Zhao Y, Cobb MH. (2007) TAO kinases mediate activation of p38 in response to DNA damage. EMBO J, 26 (8): 2005-14. [PMID:17396146]
8. 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]
9. Zhang Z, Tang Z, Ma X, Sun K, Fan L, Fang J, Pan J, Wang X, An H, Zhou J. (2018) TAOK1 negatively regulates IL-17-mediated signaling and inflammation. Cell Mol Immunol, 15 (8): 794-802. [PMID:29400705]
TAO subfamily: TAO kinase 1. Last modified on 23/01/2024. Accessed on 13/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2233.