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Target id: 2003
Nomenclature: death associated protein kinase 2
Abbreviated Name: DAPK2
Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 370 | 15q22.31 | DAPK2 | death associated protein kinase 2 | 6 |
Mouse | - | 370 | 9 35.75 cM | Dapk2 | death-associated protein kinase 2 | 6 |
Rat | - | 215 | 8 q24 | Dapk2 | death-associated protein kinase 2 |
Previous and Unofficial Names |
DRP-1 | death-associated protein kinase 2 |
Database Links | |
Alphafold | Q9UIK4 (Hs), Q8VDF3 (Mm) |
BRENDA | 2.7.11.1 |
ChEMBL Target | CHEMBL3123 (Hs) |
Ensembl Gene | ENSG00000035664 (Hs), ENSMUSG00000032380 (Mm), ENSRNOG00000017332 (Rn) |
Entrez Gene | 23604 (Hs), 13143 (Mm), 300799 (Rn) |
Human Protein Atlas | ENSG00000035664 (Hs) |
KEGG Enzyme | 2.7.11.1 |
KEGG Gene | hsa:23604 (Hs), mmu:13143 (Mm), rno:300799 (Rn) |
Pharos | Q9UIK4 (Hs) |
RefSeq Nucleotide | NM_014326 (Hs), NM_010019 (Mm), NM_001013109 (Rn) |
RefSeq Protein | NP_055141 (Hs), NP_034149 (Mm), NP_001013127 (Rn) |
UniProtKB | Q9UIK4 (Hs), Q8VDF3 (Mm) |
Wikipedia | DAPK2 (Hs) |
Enzyme Reaction | ||||
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Inhibitor Comments | ||
DAPK inhibitor 13 is a pan-DAPK inhibitor in enzyme activity assays [5,7]. |
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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Key to terms and symbols | Click column headers to sort | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Target used in screen: DAPK2 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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: 1,3 |
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Target used in screen: DAPK2/DAPK2 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Immunopharmacology Comments |
DAPk2 is recognised as a regulator of apoptosis, autophagy and inflammation [4]. DAPK2 may be a novel target for anti-inflammatory therapies due to its involvement in positively recruiting neutrophils sites of inflammation. |
Cell Type Associations | ||||||||
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Tissue Distribution | ||||||||
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Physiological Functions | ||||||||
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General Comments |
DAPK2 is a cytoplasmic Ca2+/CaM-dependent protein kinase and activity is modulated by intracellular Ca2+-concentration. Overexpression of DAPK2 induces morphological changes indicative of apoptosis [6]. |
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. Geering B. (2015) Death-associated protein kinase 2: Regulator of apoptosis, autophagy and inflammation. Int J Biochem Cell Biol, 65: 151-4. [PMID:26055515]
5. Geering B, Stoeckle C, Rozman S, Oberson K, Benarafa C, Simon HU. (2014) DAPK2 positively regulates motility of neutrophils and eosinophils in response to intermediary chemoattractants. J Leukoc Biol, 95 (2): 293-303. [PMID:24163421]
6. Kawai T, Nomura F, Hoshino K, Copeland NG, Gilbert DJ, Jenkins NA, Akira S. (1999) Death-associated protein kinase 2 is a new calcium/calmodulin-dependent protein kinase that signals apoptosis through its catalytic activity. Oncogene, 18 (23): 3471-80. [PMID:10376525]
7. Okamoto M, Takayama K, Shimizu T, Muroya A, Furuya T. (2010) Structure-activity relationship of novel DAPK inhibitors identified by structure-based virtual screening. Bioorg Med Chem, 18 (7): 2728-34. [PMID:20206532]
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]
Death-associated kinase (DAPK) family: death associated protein kinase 2. Last modified on 19/01/2017. Accessed on 04/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2003.