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calcium/calmodulin-dependent protein kinase II gamma subunit

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Target id: 1557

Nomenclature: calcium/calmodulin-dependent protein kinase II gamma subunit

Abbreviated Name: CaMK2γ

Family: CAMK2 family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 558 10q22.2 CAMK2G calcium/calmodulin dependent protein kinase II gamma
Mouse - 529 14 A3 Camk2g calcium/calmodulin-dependent protein kinase II gamma
Rat - 527 15p16 Camk2g calcium/calmodulin-dependent protein kinase II gamma
Previous and Unofficial Names Click here for help
CaMK II | CaMK-II subunit gamma | CAMKG
Database Links Click here for help
Alphafold Q13555 (Hs), Q923T9 (Mm), P11730 (Rn)
BRENDA 2.7.11.17
ChEMBL Target CHEMBL3829 (Hs), CHEMBL5109 (Rn)
Ensembl Gene ENSG00000148660 (Hs), ENSMUSG00000021820 (Mm), ENSRNOG00000009783 (Rn)
Entrez Gene 818 (Hs), 12325 (Mm), 171140 (Rn)
Human Protein Atlas ENSG00000148660 (Hs)
KEGG Enzyme 2.7.11.17
KEGG Gene hsa:818 (Hs), mmu:12325 (Mm), rno:171140 (Rn)
OMIM 602123 (Hs)
Pharos Q13555 (Hs)
RefSeq Nucleotide NM_001204492 (Hs), NM_178597 (Mm), NM_133605 (Rn)
RefSeq Protein NP_001213 (Hs), NP_848712 (Mm), NP_001034227 (Mm), NP_001034228 (Mm), NP_598289 (Rn)
UniProtKB Q13555 (Hs), Q923T9 (Mm), P11730 (Rn)
Wikipedia CAMK2G (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  STRUCTURE OF THE OLIGOMERISATION DOMAIN OF CALCIUM-CALMODULIN DEPENDENT PROTEIN KINASE II GAMMA
PDB Id:  2UX0
Resolution:  2.46Å
Species:  Human
References:  4
Image of receptor 3D structure from RCSB PDB
Description:  CRYSTAL STRUCTURE OF HUMAN CALCIUM-CALMODULIN-DEPENDENT PROTEIN KINASE II GAMMA
PDB Id:  2V7O
Resolution:  2.25Å
Species:  Human
References:  4
Enzyme Reaction Click here for help
EC Number: 2.7.11.17

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
bosutinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.7 pIC50 5
⤷ pIC50 6.7 (IC50 1.84x10-7 M) [5]
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: 2,6
Key to terms and symbols Click column headers to sort
Target used in screen: CAMK2G
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.3 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.6 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.0 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.8 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.1 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.1 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.0 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.0 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: 1,3
Key to terms and symbols Click column headers to sort
Target used in screen: CaMKIIγ/CAMK2g
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 0.7 0.5 -3.5
K-252a Small molecule or natural product Hs Inhibitor Inhibition 3.1 1.0 0.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.1 3.0 0.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 8.4 0.0 1.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 15.6 2.0 0.0
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 21.9 2.0 -5.0
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 25.1
GSK-3 inhibitor IX Small molecule or natural product Hs Inhibitor Inhibition 28.3 3.0 2.0
indirubin derivative E804 Small molecule or natural product Hs Inhibitor Inhibition 35.3 6.0 0.0
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 43.9 10.0 -1.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Cytokine production & signalling

References

Show »

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. 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]

5. Remsing Rix LL, Rix U, Colinge J, Hantschel O, Bennett KL, Stranzl T, Müller A, Baumgartner C, Valent P, Augustin M et al.. (2009) Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. Leukemia, 23 (3): 477-85. [PMID:19039322]

6. 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]

How to cite this page

CAMK2 family: calcium/calmodulin-dependent protein kinase II gamma subunit. Last modified on 13/02/2017. Accessed on 10/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1557.