calcium/calmodulin-dependent protein kinase II gamma subunit

Target id: 1557

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

Abbreviated Name: CaMK2γ

Family: CAMK2 family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for calcium/calmodulin-dependent protein kinase II gamma subunit in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 495 10q22 CAMK2G calcium/calmodulin dependent protein kinase II gamma
Mouse - 529 14 Camk2g calcium/calmodulin-dependent protein kinase II gamma
Rat - 527 15p16 Camk2g calcium/calmodulin-dependent protein kinase II gamma
Previous and Unofficial Names
CaMK II | CaMK-II subunit gamma | CAMKG
Database Links
BRENDA
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
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
EC Number: 2.7.11.17

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
Ligand Sp. Action Affinity Units Reference
bosutinib Hs Inhibition 6.7 pIC50 5
pIC50 6.7 (IC50 1.84x10-7 M) [5]
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: 2,6

Key to terms and symbols Click column headers to sort
Target used in screen: CAMK2G
Ligand Sp. Type Action Affinity Units
staurosporine Hs Inhibitor Inhibition 9.3 pKd
lestaurtinib Hs Inhibitor Inhibition 7.6 pKd
ruxolitinib Hs Inhibitor Inhibition 7.0 pKd
midostaurin Hs Inhibitor Inhibition 6.8 pKd
fedratinib Hs Inhibitor Inhibition 6.3 pKd
sunitinib Hs Inhibitor Inhibition 6.2 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.1 pKd
A-674563 Hs Inhibitor Inhibition 6.1 pKd
tamatinib Hs Inhibitor Inhibition 6.0 pKd
SU-14813 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
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 Hs Inhibitor Inhibition 0.7 0.5 -3.5
K-252a Hs Inhibitor Inhibition 3.1 1.0 0.0
SU11652 Hs Inhibitor Inhibition 8.1 3.0 0.0
SB 218078 Hs Inhibitor Inhibition 8.4 0.0 1.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 15.6 2.0 0.0
Gö 6976 Hs Inhibitor Inhibition 21.9 2.0 -5.0
sunitinib Hs Inhibitor Inhibition 25.1
GSK-3 inhibitor IX Hs Inhibitor Inhibition 28.3 3.0 2.0
indirubin derivative E804 Hs Inhibitor Inhibition 35.3 6.0 0.0
midostaurin Hs Inhibitor Inhibition 43.9 10.0 -1.0
Displaying the top 10 most potent ligands  View all ligands in screen »

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 15/07/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1557.