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Calmodulin-dependent kinase II

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Target id: 1554

Nomenclature: Calmodulin-dependent kinase II

Abbreviated Name: CaMKII

Family: CAMK2 family

Contents:

Database Links Click here for help
BRENDA 2.7.11.17
KEGG Enzyme 2.7.11.17
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Full-length human CaMKII
PDB Id:  3SOA
Resolution:  3.55Å
Species:  Human
References:  1
Enzyme Reaction Click here for help
EC Number: 2.7.11.17

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Activators
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
calmodulin {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Activation - -
⤷
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 20 [PMID: 22136433] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.1 pIC50 3
⤷ pIC50 7.1 (IC50 8.3x10-8 M) [3]
KN62 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 6.1 pIC50 4
⤷ pIC50 6.1 (IC50 9x10-7 M) [4]
K-252a Small molecule or natural product Click here for species-specific activity table Hs Inhibition - - 2
⤷ [2]
General Comments
Camodulin-dependent kinase II is a homo- or heterotromultimeric holoenzyme made up of 8 to 12 subunit chains.

References

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1. Chao LH, Stratton MM, Lee IH, Rosenberg OS, Levitz J, Mandell DJ, Kortemme T, Groves JT, Schulman H, Kuriyan J. (2011) A mechanism for tunable autoinhibition in the structure of a human Ca2+/calmodulin- dependent kinase II holoenzyme. Cell, 146 (5): 732-45. [PMID:21884935]

2. Hashimoto Y, Nakayama T, Teramoto T, Kato H, Watanabe T, Kinoshita M, Tsukamoto K, Tokunaga K, Kurokawa K, Nakanishi S. (1991) Potent and preferential inhibition of Ca2+/calmodulin-dependent protein kinase II by K252a and its derivative, KT5926. Biochem Biophys Res Commun, 181 (1): 423-9. [PMID:1659814]

3. Huber K, Brault L, Fedorov O, Gasser C, Filippakopoulos P, Bullock AN, Fabbro D, Trappe J, Schwaller J, Knapp S et al.. (2012) 7,8-dichloro-1-oxo-β-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes. J Med Chem, 55 (1): 403-13. [PMID:22136433]

4. Tokumitsu H, Chijiwa T, Hagiwara M, Mizutani A, Terasawa M, Hidaka H. (1990) KN-62, 1-[N,O-bis(5-isoquinolinesulfonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazi ne, a specific inhibitor of Ca2+/calmodulin-dependent protein kinase II. J Biol Chem, 265 (8): 4315-20. [PMID:2155222]

How to cite this page

CAMK2 family: Calmodulin-dependent kinase II. Last modified on 13/02/2015. Accessed on 15/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1554.