phosphatidylinositol-4-phosphate 5-kinase type 1 alpha

Target id: 2164

Nomenclature: phosphatidylinositol-4-phosphate 5-kinase type 1 alpha

Abbreviated Name: PIP5K1A

Family: Type I PIP kinases (1-phosphatidylinositol-4-phosphate 5-kinase family), Phosphatidylinositol phosphate 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-phosphate 5-kinase type 1 alpha in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 549 1q21.3 PIP5K1A phosphatidylinositol-4-phosphate 5-kinase type 1 alpha 4,7
Mouse - 546 3 F2.1 Pip5k1a phosphatidylinositol-4-phosphate 5-kinase
Rat - 546 2 q34 Pip5k1a phosphatidylinositol-4-phosphate 5-kinase
Previous and Unofficial Names
PIP5K1-alpha | Pipk5a | phosphatidylinositol-4-phosphate 5-kinase, type 1, alpha | phosphatidylinositol-4-phosphate 5-kinase, type I, alpha | phosphatidylinositol-4-phosphate 5-kinase | phosphatidylinositol-4-phosphate 5-kinase, type 1 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: 2.7.1.68

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
ISA-2011B Hs Inhibition - - 5
[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: PIP5K1A
Ligand Sp. Type Action Affinity Units
lestaurtinib Hs Inhibitor Inhibition 7.4 pKd
staurosporine Hs Inhibitor Inhibition 7.4 pKd
KW-2449 Hs Inhibitor Inhibition 7.3 pKd
fedratinib Hs Inhibitor Inhibition 7.2 pKd
SU-14813 Hs Inhibitor Inhibition 6.9 pKd
tozasertib Hs Inhibitor Inhibition 6.9 pKd
A-674563 Hs Inhibitor Inhibition 6.6 pKd
PHA-665752 Hs Inhibitor Inhibition 6.6 pKd
midostaurin Hs Inhibitor Inhibition 6.5 pKd
JNJ-28312141 Hs Inhibitor Inhibition 6.2 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Physiological Functions
Pip5k1a is required for the maintenance of sperm number and morphology during spermatogenesis in mice.
Species:  Mouse
Tissue:  Seminiferous tubules and sperm.
References:  3
PIP5K1A is an upstream regulator of the small GTPase Rac1, and plays a role in regulating cell migration.
Species:  Human
Tissue:  HeLa cells
References:  1
PIP5K1A is necessary for random and directional cell migration (eg migration induced in response to a chemotactic stimulus, in this case a PDGF gradient).
Species:  Human
Tissue:  HT1080 cells with PIP5K1A knock-down.
References:  1
Physiological Consequences of Altering Gene Expression
Pip5k1a knockout mice are subfertile (Pip5k1a only) or infertile (double knockout of Pip5k1a and Pip5k1b).
Species:  Mouse
Tissue:  Seminiferous tubules and sperm.
Technique:  Gene knock-outs.
References:  3

References

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1. Chao WT, Daquinag AC, Ashcroft F, Kunz J. (2010) Type I PIPK-alpha regulates directed cell migration by modulating Rac1 plasma membrane targeting and activation. J. Cell Biol.190 (2): 247-62. [PMID:20660631]

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. Hasegawa H, Noguchi J, Yamashita M, Okada R, Sugimoto R, Furuya M, Unoki T, Funakoshi Y, Baba T, Kanaho Y. (2012) Phosphatidylinositol 4-phosphate 5-kinase is indispensable for mouse spermatogenesis. Biol. Reprod.86 (5): 136, 1-12. [PMID:22321832]

4. Loijens JC, Anderson RA. (1996) Type I phosphatidylinositol-4-phosphate 5-kinases are distinct members of this novel lipid kinase family. J. Biol. Chem.271 (51): 32937-43. [PMID:8955136]

5. Semenas J, Hedblom A, Miftakhova RR, Sarwar M, Larsson R, Shcherbina L, Johansson ME, Härkönen P, Sterner O, Persson JL. (2014) The role of PI3K/AKT-related PIP5K1α and the discovery of its selective inhibitor for treatment of advanced prostate cancer. Proc. Natl. Acad. Sci. U.S.A.111 (35): E3689-98. [PMID:25071204]

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]

7. Xie Y, Zhu L, Zhao G. (2000) Assignment of type I phosphatidylinositol-4-phosphate 5-kinase (PIP5K1A) to human chromosome bands 1q22--> q24 by in situ hybridization. Cytogenet. Cell Genet.88 (3-4): 197-9. [PMID:10828584]

How to cite this page

Phosphatidylinositol phosphate kinases: phosphatidylinositol-4-phosphate 5-kinase type 1 alpha. Last modified on 19/08/2015. Accessed on 15/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2164.