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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

Contents:

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 Q99755 (Hs), P70182 (Mm)
BRENDA 2.7.1.68
CATH/Gene3D 3.30.800.10, 3.30.810.10
ChEMBL Target CHEMBL5969 (Hs)
Ensembl Gene ENSG00000143398 (Hs), ENSMUSG00000028126 (Mm), ENSRNOG00000021068 (Rn)
Entrez Gene 8394 (Hs), 18720 (Mm), 365865 (Rn)
Human Protein Atlas ENSG00000143398 (Hs)
KEGG Enzyme 2.7.1.68
KEGG Gene hsa:8394 (Hs), mmu:18720 (Mm), rno:365865 (Rn)
OMIM 603275 (Hs)
Pharos Q99755 (Hs)
RefSeq Nucleotide NM_003557 (Hs), NM_008847 (Mm), NM_001042621 (Rn)
RefSeq Protein NP_003548 (Hs), NP_032873 (Mm), NP_001036086 (Rn)
UniProtKB Q99755 (Hs), P70182 (Mm)
Wikipedia PIP5K1A (Hs)
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 Ligand has a PDB structure 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 »
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

Phosphatidylinositol phosphate kinases: phosphatidylinositol-4-phosphate 5-kinase type 1 alpha. Last modified on 19/08/2015. Accessed on 04/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2164.