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phosphatidylinositol-4-phosphate 5-kinase type 1 gamma

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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

Contents:

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 O60331 (Hs), O70161 (Mm), Q5I6B8 (Rn)
BRENDA 2.7.1.68
CATH/Gene3D 3.30.800.10, 3.30.810.10
ChEMBL Target CHEMBL1908383 (Hs)
Ensembl Gene ENSG00000186111 (Hs), ENSMUSG00000034902 (Mm), ENSRNOG00000020577 (Rn)
Entrez Gene 23396 (Hs), 18717 (Mm), 314641 (Rn)
Human Protein Atlas ENSG00000186111 (Hs)
KEGG Enzyme 2.7.1.68
KEGG Gene hsa:23396 (Hs), mmu:18717 (Mm), rno:314641 (Rn)
OMIM 606102 (Hs)
Orphanet ORPHA160322 (Hs)
Pharos O60331 (Hs)
RefSeq Nucleotide NM_001195733 (Hs), NM_001146687 (Mm), NM_001033970 (Rn)
RefSeq Protein NP_036530 (Hs), NP_001140159 (Mm), NP_001029142 (Rn)
UniProtKB O60331 (Hs), O70161 (Mm), Q5I6B8 (Rn)
Wikipedia PIP5K1C (Hs)
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
Immuno Process:  Antigen presentation
Immuno Process:  Chemotaxis & migration
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

Phosphatidylinositol phosphate kinases: phosphatidylinositol-4-phosphate 5-kinase type 1 gamma. Last modified on 13/08/2015. Accessed on 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2165.