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phosphatidylinositol-4-phosphate 5-kinase type 1 alpha

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Target not currently curated in GtoImmuPdb

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

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 562 1q21.3 PIP5K1A phosphatidylinositol-4-phosphate 5-kinase type 1 alpha 4,7
Mouse - 546 3 F2.1 Pip5k1a phosphatidylinositol-4-phosphate 5-kinase, type 1 alpha
Rat - 546 2 q34 Pip5k1a phosphatidylinositol-4-phosphate 5-kinase, type 1, alpha
Previous and Unofficial Names Click here for help
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 Click here for help
Alphafold
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 2.7.1.68

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
ISA-2011B Small molecule or natural product Primary target of this compound Hs Inhibition - - 5
[5]
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: 2,6

Key to terms and symbols Click column headers to sort
Target used in screen: PIP5K1A
Ligand Sp. Type Action Value Parameter
lestaurtinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 7.4 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 7.3 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.9 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.9 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
PHA-665752 Small molecule or natural product Hs Inhibitor Inhibition 6.6 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.5 pKd
JNJ-28312141 Small molecule or natural product Hs Inhibitor Inhibition 6.2 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes
GO:0006909 phagocytosis TAS
Physiological Functions Click here for help
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
Pip5k1a is required for the maintenance of sperm number and morphology during spermatogenesis in mice.
Species:  Mouse
Tissue:  Seminiferous tubules and sperm.
References:  3
Physiological Consequences of Altering Gene Expression Click here for help
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 USA, 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

Type I PIP kinases (1-phosphatidylinositol-4-phosphate 5-kinase family): phosphatidylinositol-4-phosphate 5-kinase type 1 alpha. Last modified on 19/08/2015. Accessed on 27/09/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2164.