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calcium/calmodulin dependent protein kinase IV

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Target id: 1955

Nomenclature: calcium/calmodulin dependent protein kinase IV

Abbreviated Name: CaMK4

Family: CAMK1 family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 473 5q22.1 CAMK4 calcium/calmodulin dependent protein kinase IV
Mouse - 469 18 18.15 cM Camk4 calcium/calmodulin-dependent protein kinase IV
Rat - 474 18p12 Camk4 calcium/calmodulin-dependent protein kinase IV
Previous and Unofficial Names Click here for help
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 Click here for help
Alphafold Q16566 (Hs), P08414 (Mm), P13234 (Rn)
BRENDA 2.7.11.17
ChEMBL Target CHEMBL2494 (Hs)
Ensembl Gene ENSG00000152495 (Hs), ENSMUSG00000038128 (Mm), ENSRNOG00000020478 (Rn)
Entrez Gene 814 (Hs), 12326 (Mm), 25050 (Rn)
Human Protein Atlas ENSG00000152495 (Hs)
KEGG Enzyme 2.7.11.17
KEGG Gene hsa:814 (Hs), mmu:12326 (Mm), rno:25050 (Rn)
OMIM 114080 (Hs)
Pharos Q16566 (Hs)
RefSeq Nucleotide NM_001744 (Hs), NM_009793 (Mm), NM_012727 (Rn)
RefSeq Protein NP_001735 (Hs), NP_033923 (Mm), NP_036859 (Rn)
UniProtKB Q16566 (Hs), P08414 (Mm), P13234 (Rn)
Wikipedia CAMK4 (Hs)
Selected 3D Structures Click here for help
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 Click here for help
EC Number: 2.7.11.17
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: 2,5
Key to terms and symbols Click column headers to sort
Target used in screen: CAMK4
Ligand Sp. Type Action Value Parameter
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.5 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
GSK-1838705A Small molecule or natural product Hs Inhibitor Inhibition 6.3 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.1 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 5.6 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure 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 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: CaMKIV/CAMK4
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 34.8 2.5 0.5
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 81.8 1.0 0.0
PDK1/Akt/Flt dual pathway inhibitor Small molecule or natural product Hs Inhibitor Inhibition 85.4 122.0 113.0
GSK-3 inhibitor X Small molecule or natural product Hs Inhibitor Inhibition 86.1 100.0 90.0
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 88.1 100.0 58.0
fascaplysin Small molecule or natural product Hs Inhibitor Inhibition 88.3 102.0 93.0
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 88.6
alsterpaullone Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 89.2 114.0 94.0
GF109203X Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 89.5 88.0 45.0
seliciclib Small molecule or natural product Ligand has a PDB structure 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
Immuno Process:  T cell (activation)
Immuno Process:  Immune regulation
Immuno Process:  Immune system development
Immuno Process:  Cellular signalling
Immuno Process:  B cell (activation)

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 20/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1955.