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Target not currently curated in GtoImmuPdb
Target id: 1555
Nomenclature: calcium/calmodulin-dependent protein kinase II alpha subunit
Abbreviated Name: CaMK2α
Family: CAMK2 family
Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 478 | 5q32 | CAMK2A | calcium/calmodulin dependent protein kinase II alpha | |
Mouse | - | 478 | 18 34.41 cM | Camk2a | calcium/calmodulin-dependent protein kinase II alpha | |
Rat | - | 478 | 18q12.1 | Camk2a | calcium/calmodulin-dependent protein kinase II alpha |
Previous and Unofficial Names |
CaM kinase II alpha subunit | CaMK-II alpha subunit | alpha CaM kinase II | PK2CDD | PKCCD | CaMKII |
Database Links | |
Alphafold | Q9UQM7 (Hs), P11798 (Mm), P11275 (Rn) |
BRENDA | 2.7.11.17 |
ChEMBL Target | CHEMBL4147 (Hs), CHEMBL2359 (Rn) |
Ensembl Gene | ENSG00000070808 (Hs), ENSMUSG00000024617 (Mm), ENSRNOG00000018712 (Rn) |
Entrez Gene | 815 (Hs), 12322 (Mm), 25400 (Rn) |
Human Protein Atlas | ENSG00000070808 (Hs) |
KEGG Enzyme | 2.7.11.17 |
KEGG Gene | hsa:815 (Hs), mmu:12322 (Mm), rno:25400 (Rn) |
OMIM | 114078 (Hs) |
Pharos | Q9UQM7 (Hs) |
RefSeq Nucleotide | NM_015981 (Hs), NM_177407 (Mm), NM_012920 (Rn) |
RefSeq Protein | NP_057065 (Hs), NP_803126 (Mm), NP_037052 (Rn) |
UniProtKB | Q9UQM7 (Hs), P11798 (Mm), P11275 (Rn) |
Wikipedia | CAMK2A (Hs) |
Selected 3D Structures | |||||||||||
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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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View species-specific inhibitor tables | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Inhibitor Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
KN-93 is a calmodulin-competitive inhibitor of CaMKII phosphorylating activity [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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Target used in screen: CAMK2A | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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 |
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Target used in screen: nd/CAMK2a | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Immuno Process Associations | ||
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General Comments |
Using photoaffinity labeling, chemoproteomics and x-ray crystallography, CaMKIIα has been identified as a specific high-affinity molecular target for the natural substance γ-hydroxybutyric acid (γ-hydroxybutyrate; GHB) and related compounds [4]. GHB-like ligand interactions with CaMKIIα induce a neuroprotective effect. |
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. Komiya M, Asano S, Koike N, Koga E, Igarashi J, Nakatani S, Isobe Y. (2011) Structure and activity relationship of 2-(substituted benzoyl)-hydroxyindoles as novel CaMKII inhibitors. Bioorg Med Chem Lett, 21 (5): 1456-8. [PMID:21292482]
4. Leurs U, Klein AB, McSpadden ED, Griem-Krey N, Solbak SMØ, Houlton J, Villumsen IS, Vogensen SB, Hamborg L, Gauger SJ et al.. (2021) GHB analogs confer neuroprotection through specific interaction with the CaMKIIα hub domain. Proc Natl Acad Sci U S A, 118 (31). [PMID:34330837]
5. Mirzoeva S, Sawkar A, Zasadzki M, Guo L, Velentza AV, Dunlap V, Bourguignon JJ, Ramstrom H, Haiech J, Van Eldik LJ et al.. (2002) Discovery of a 3-amino-6-phenyl-pyridazine derivative as a new synthetic antineuroinflammatory compound. J Med Chem, 31 (45): 563-6. [PMID:11806708]
6. Rellos P, Pike AC, Niesen FH, Salah E, Lee WH, von Delft F, Knapp S. (2010) Structure of the CaMKIIdelta/calmodulin complex reveals the molecular mechanism of CaMKII kinase activation. PLoS Biol, 8 (7): e1000426. [PMID:20668654]
7. Sumi M, Kiuchi K, Ishikawa T, Ishii A, Hagiwara M, Nagatsu T, Hidaka H. (1991) The newly synthesized selective Ca2+/calmodulin dependent protein kinase II inhibitor KN-93 reduces dopamine contents in PC12h cells. Biochem Biophys Res Commun, 181 (3): 968-75. [PMID:1662507]
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]
CAMK2 family: calcium/calmodulin-dependent protein kinase II alpha subunit. Last modified on 01/05/2023. Accessed on 08/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1555.