calcium/calmodulin-dependent serine protein kinase (MAGUK family)

Target id: 1959

Nomenclature: calcium/calmodulin-dependent serine protein kinase (MAGUK family)

Abbreviated Name: CASK

Family: CASK 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 - 898 Xp11.4 CASK calcium/calmodulin-dependent serine protein kinase (MAGUK family)
Mouse - 897 X A1.1 Cask calcium/calmodulin-dependent serine protein kinase (MAGUK family)
Rat - 909 Xq12 Cask calcium/calmodulin-dependent serine protein kinase (MAGUK family)
Previous and Unofficial Names
CAGH39
FGS4
LIN2
Pals3
peripheral plasma membrane protein CASK
TNRC8
trinucleotide repeat containing 8
Database Links
BRENDA
Ensembl Gene
Entrez Gene
ExplorEnz
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG BRITE Hierarchy
KEGG Gene
OMIM
Orphanet Gene
PhosphoSitePlus
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of the Guanylate Kinase-like Domain of Human CASK
PDB Id:  1KGD
Resolution:  1.31Å
Species:  Human
References:  2
Enzyme Reaction
EC Number: 2.7.11.1
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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: CASK
Ligand Sp. Type Action Affinity Units
staurosporine Hs Inhibitor Inhibition 7.72 pKd
AT-7519 Hs Inhibitor Inhibition 7.62 pKd
R547 Hs Inhibitor Inhibition 7.18 pKd
crizotinib Hs Inhibitor Inhibition 6.85 pKd
lestaurtinib Hs Inhibitor Inhibition 6.48 pKd
BMS-387032 Hs Inhibitor Inhibition 6.4 pKd
bosutinib Hs Inhibitor Inhibition 6.08 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.04 pKd
ruxolitinib Hs Inhibitor Inhibition 5.82 pKd
PP-242 Hs Inhibitor Inhibition 5.8 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology
Disease:  FG syndrome 4
OMIM:  300422
Disease:  Mental retardation and microcephaly with pontine and cerebellar hypoplasia
OMIM:  300749
Orphanet:  163937

References

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1. 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]

2. Li Y, Spangenberg O, Paarmann I, Konrad M, Lavie A. (2002) Structural basis for nucleotide-dependent regulation of membrane-associated guanylate kinase-like domains. J. Biol. Chem.277 (6): 4159-65. [PMID:11729206]

3. 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

CASK family: calcium/calmodulin-dependent serine protein kinase (MAGUK family). Last modified on 21/03/2014. Accessed on 22/12/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1959.