phosphatidylinositol 4-kinase alpha

Target id: 2148

Nomenclature: phosphatidylinositol 4-kinase alpha

Abbreviated Name: PI4KIIIα/PIK4CA

Family: 1-phosphatidylinositol 4-kinase family, Phosphatidylinositol kinases

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 phosphatidylinositol 4-kinase alpha in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 2102 22q11.21 PI4KA phosphatidylinositol 4-kinase alpha
Mouse - 2044 16 A3 Pi4ka phosphatidylinositol 4-kinase alpha
Rat - 2041 11 q23 Pi4ka phosphatidylinositol 4-kinase alpha
Previous and Unofficial Names
phosphatidylinositol 4-kinase, catalytic, alpha | leuserpin 2 | PI4K-alpha | PtdIns-4-kinase alpha
Database Links
BRENDA
CATH/Gene3D
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.1.67

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
wortmannin Hs Inhibition 6.7 – 6.8 pIC50 3,5
pIC50 6.7 – 6.8 [3,5]
phenylarsine oxide Hs Inhibition - - 1
[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: 2,6

Key to terms and symbols Click column headers to sort
Target used in screen: PIK4CB
Ligand Sp. Type Action Affinity Units
MLN-120B Hs Inhibitor Inhibition 6.6 pKd
lestaurtinib Hs Inhibitor Inhibition 6.5 pKd
TG-100-115 Hs Inhibitor Inhibition 6.4 pKd
staurosporine Hs Inhibitor Inhibition 6.3 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.1 pKd
tamatinib Hs Inhibitor Inhibition 6.0 pKd
PP-242 Hs Inhibitor Inhibition 6.0 pKd
lapatinib Hs Inhibitor Inhibition 6.0 pKd
pazopanib Hs Inhibitor Inhibition 6.0 pKd
PLX-4720 Hs Inhibitor Inhibition 5.9 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Tissue Distribution
Intracellular membranes, with prominent co-localization with early endosomes and recycling endosomes but not with the Golgi.
Species:  Human
Technique:  Immunocytochemistry and confocal microscopy using epitope-tagged and green fluorescent protein-tagged enzyme expressed in COS-7 cells.
References:  1
Physiological Functions
PI4KIIα is required for trafficking LIMP-2 (a receptor for transport of β-glucocerebrosidase into lysosomes) at a post-Golgi compartment (endocytic transport), leading to accumulation of LIMP-2 in enlarged endosomal vesicles. β-glucocerebrosidase (GBA) is the Gaucher disease enzyme.
Species:  Human
Tissue:  COS-7 cells transfected with a fluorescent LIMP-2.
References:  4

References

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1. Balla A, Tuymetova G, Barshishat M, Geiszt M, Balla T. (2002) Characterization of type II phosphatidylinositol 4-kinase isoforms reveals association of the enzymes with endosomal vesicular compartments. J. Biol. Chem.277 (22): 20041-50. [PMID:11923287]

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. Gehrmann T, Gülkan H, Suer S, Herberg FW, Balla A, Vereb G, Mayr GW, Heilmeyer Jr LM. (1999) Functional expression and characterisation of a new human phosphatidylinositol 4-kinase PI4K230. Biochim. Biophys. Acta1437 (3): 341-56. [PMID:10101268]

4. Jović M, Kean MJ, Szentpetery Z, Polevoy G, Gingras AC, Brill JA, Balla T. (2012) Two phosphatidylinositol 4-kinases control lysosomal delivery of the Gaucher disease enzyme, β-glucocerebrosidase. Mol. Biol. Cell23 (8): 1533-45. [PMID:22337770]

5. Meyers R, Cantley LC. (1997) Cloning and characterization of a wortmannin-sensitive human phosphatidylinositol 4-kinase. J. Biol. Chem.272 (7): 4384-90. [PMID:9020160]

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

Phosphatidylinositol kinases: phosphatidylinositol 4-kinase alpha. Last modified on 06/06/2016. Accessed on 23/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2148.