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phosphatidylinositol-4-phosphate 5-kinase type 1 gamma

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Target not currently curated in GtoImmuPdb

Target id: 2165

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

Abbreviated Name: PIP5K1C

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 - 668 19p13.3 PIP5K1C phosphatidylinositol-4-phosphate 5-kinase type 1 gamma
Mouse - 661 10 C1 Pip5k1c phosphatidylinositol-4-phosphate 5-kinase, type 1 gamma
Rat - 688 7q11 Pip5k1c phosphatidylinositol-4-phosphate 5-kinase type 1 gamma
Previous and Unofficial Names Click here for help
PIP5K1-gamma | phosphatidylinositol-4-phosphate 5-kinase, type I, gamma | phosphatidylinositol-4-phosphate 5-kinase
Database Links Click here for help
Alphafold
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Molecular basis for the association of PIPKIgamma -p90 with the clathrin adaptor AP-2
PDB Id:  3H1Z
Resolution:  1.83Å
Species:  Human
References:  2
Enzyme Reaction Click here for help
EC Number: 2.7.1.68
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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: PIP5K1C
Ligand Sp. Type Action Value Parameter
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.9 pKd
TG-100-115 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.8 pKd
pazopanib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 5.7 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 5.6 pKd
alvocidib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.6 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.6 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 2 GO processes
GO:0006909 phagocytosis TAS
GO:0030593 neutrophil chemotaxis TAS
Immuno Process:  Antigen presentation
GO Annotations:  Associated to 5 GO processes
GO:0048488 synaptic vesicle endocytosis TAS
GO:0072583 clathrin-dependent endocytosis TAS
GO:0099149 regulation of postsynaptic neurotransmitter receptor internalization IDA
GO:1900242 regulation of synaptic vesicle endocytosis IDA
click arrow to show/hide IEA associations
GO:0006897 endocytosis IEA
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 1 GO processes
GO:0030593 neutrophil chemotaxis TAS
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Lethal congenital contractural syndrome 3; LCCS3
OMIM: 611369
Orphanet: ORPHA137783

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. Kahlfeldt N, Vahedi-Faridi A, Koo SJ, Schäfer JG, Krainer G, Keller S, Saenger W, Krauss M, Haucke V. (2010) Molecular basis for association of PIPKI gamma-p90 with clathrin adaptor AP-2. J Biol Chem, 285 (4): 2734-49. [PMID:19903820]

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

Type I PIP kinases (1-phosphatidylinositol-4-phosphate 5-kinase family): phosphatidylinositol-4-phosphate 5-kinase type 1 gamma. Last modified on 13/08/2015. Accessed on 20/09/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2165.