phosphatidylinositol-4-phosphate 5-kinase type 1 gamma

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

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 gamma in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 668 19p13.3 PIP5K1C phosphatidylinositol-4-phosphate 5-kinase type 1 gamma
Mouse - 635 19 C1 Pip5k1c phosphatidylinositol-4-phosphate 5-kinase, type 1 gamma
Rat - 636 7q11 Pip5k1c phosphatidylinositol-4-phosphate 5-kinase type 1 gamma
Previous and Unofficial Names
PIP5K1-gamma | phosphatidylinositol-4-phosphate 5-kinase, type I, gamma | phosphatidylinositol-4-phosphate 5-kinase
Database Links
BRENDA
CATH/Gene3D
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
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
EC Number: 2.7.1.68
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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: PIP5K1C
Ligand Sp. Type Action Affinity Units
PP-242 Hs Inhibitor Inhibition 7.7 pKd
tamatinib Hs Inhibitor Inhibition 6.9 pKd
TG-100-115 Hs Inhibitor Inhibition 6.5 pKd
ruboxistaurin Hs Inhibitor Inhibition 6.3 pKd
GSK690693 Hs Inhibitor Inhibition 5.8 pKd
pazopanib Hs Inhibitor Inhibition 5.7 pKd
SB203580 Hs Inhibitor Inhibition 5.6 pKd
alvocidib Hs Inhibitor Inhibition 5.6 pKd
staurosporine Hs Inhibitor Inhibition 5.6 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology
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

Phosphatidylinositol phosphate kinases: phosphatidylinositol-4-phosphate 5-kinase type 1 gamma. Last modified on 13/08/2015. Accessed on 24/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2165.