calcium/calmodulin dependent protein kinase IV | CAMK1 family | IUPHAR Guide to IMMUNOPHARMACOLOGY

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calcium/calmodulin dependent protein kinase IV

  Target has curated data in GtoImmuPdb

Target id: 1955

Nomenclature: calcium/calmodulin dependent protein kinase IV

Abbreviated Name: CaMK4

Family: CAMK1 family

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 473 5q21.3 CAMK4 calcium/calmodulin dependent protein kinase IV
Mouse - 469 18 B1 Camk4 calcium/calmodulin-dependent protein kinase IV
Rat - 474 18p12 Camk4 calcium/calmodulin-dependent protein kinase IV
Previous and Unofficial Names
brain Ca++-calmodulin-dependent protein kinase type IV | Ca2+/calmodulin-dependent protein kinase type IV/Gr | calspermin | CAM kinase IV | CAM kinase-GR | caMK IV
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:  Crystal structure of Human CAMK4 in complex with 4-Amino(sulfamoyl- phenylamino)-triazole-carbothioic acid (2,6-difluoro-phenyl)-amide)
PDB Id:  2W4O
Resolution:  2.17Å
Species:  Human
References: 
Enzyme Reaction
EC Number: 2.7.11.17
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: 2,5

Key to terms and symbols Click column headers to sort
Target used in screen: CAMK4
Ligand Sp. Type Action Affinity Parameter
NVP-TAE684 Hs Inhibitor Inhibition 7.5 pKd
staurosporine Hs Inhibitor Inhibition 7.4 pKd
GSK690693 Hs Inhibitor Inhibition 6.4 pKd
GSK-1838705A Hs Inhibitor Inhibition 6.3 pKd
A-674563 Hs Inhibitor Inhibition 6.2 pKd
sunitinib Hs Inhibitor Inhibition 6.1 pKd
SU-14813 Hs Inhibitor Inhibition 5.6 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 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: CaMKIV/CAMK4
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 34.8 2.5 0.5
JAK inhibitor I Hs Inhibitor Inhibition 81.8 1.0 0.0
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 85.4 122.0 113.0
GSK-3 inhibitor X Hs Inhibitor Inhibition 86.1 100.0 90.0
Gö 6976 Hs Inhibitor Inhibition 88.1 100.0 58.0
fascaplysin Hs Inhibitor Inhibition 88.3 102.0 93.0
sunitinib Hs Inhibitor Inhibition 88.6
alsterpaullone Hs Inhibitor Inhibition 89.2 114.0 94.0
GF109203X Hs Inhibitor Inhibition 89.5 88.0 45.0
seliciclib Hs Inhibitor Inhibition 89.6
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
CAMKIV has been implicated in the differentiation of Th17 cells, suggesting CAMKIV as a target for therapeutic intervention in Th17-driven autoimmune diseases [4].
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 2 GO processes
GO:0043011 myeloid dendritic cell differentiation IMP
click arrow to show/hide IEA associations
GO:0006954 inflammatory response IEA
Immuno Process:  T cell (activation)
GO Annotations:  Associated to 2 GO processes
GO:0033081 regulation of T cell differentiation in thymus TAS
click arrow to show/hide IEA associations
GO:0002250 adaptive immune response IEA
Immuno Process:  Immune regulation
GO Annotations:  Associated to 2 GO processes
GO:0033081 regulation of T cell differentiation in thymus TAS
GO:0045670 regulation of osteoclast differentiation TAS
Immuno Process:  Immune system development
GO Annotations:  Associated to 3 GO processes
GO:0033081 regulation of T cell differentiation in thymus TAS
GO:0043011 myeloid dendritic cell differentiation IMP
GO:0045670 regulation of osteoclast differentiation TAS
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 1 GO processes
GO:0033081 regulation of T cell differentiation in thymus TAS
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 2 GO processes
GO:0033081 regulation of T cell differentiation in thymus TAS
GO:0043011 myeloid dendritic cell differentiation IMP
Immuno Process:  B cell (activation)
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0002250 adaptive immune response IEA

References

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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. Koga T, Hedrich CM, Mizui M, Yoshida N, Otomo K, Lieberman LA, Rauen T, Crispín JC, Tsokos GC. (2014) CaMK4-dependent activation of AKT/mTOR and CREM-α underlies autoimmunity-associated Th17 imbalance. J. Clin. Invest., 124 (5): 2234-45. [PMID:24667640]

5. 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

CAMK1 family: calcium/calmodulin dependent protein kinase IV. Last modified on 16/02/2017. Accessed on 16/02/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1955.