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Information on EC 2.7.1.150 - 1-phosphatidylinositol-3-phosphate 5-kinase and Organism(s) Homo sapiens
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2.7.1.150 1-phosphatidylinositol-3-phosphate 5-kinaseSpecify your search results
Word Map
- 2.7.1.150
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mating
- pheromone
- vacuole
- endosomal
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ptdins3,5p2
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haploid
- 3,5-bisphosphate
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ptdins5p
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endolysosomal
- apilimod
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pheromone-induced
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pseudohyphal
- phosphatidylinositol-3,5-bisphosphate
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pheromone-responsive
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charcot-marie-tooth
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mating-type
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mating-specific
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fleck
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alpha-specific
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matalpha
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a-specific
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trpml1
- a-factor
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insulin-regulated
- drug development
The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
The enzyme appears in selected viruses and cellular organisms
Reaction Schemes
Synonyms
pikfyve, ste12, fab1p, pip5k3, fab1/pikfyve, phosphatidylinositol 3-phosphate 5-kinase, ppk-3, phosphatidylinositol-3-phosphate-5-kinase pikfyve, ptdins3p 5-kinase, cgfab1, 
more
topSYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
Fab1p
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kinase (phosphorylating), phosphatidylinositol 3-phosphate 5-
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phosphatidylinositol 3-phosphate 5-kinase
Phosphatidylinositol-3-phosphate 5-kinase
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PI(3)P-5-kinase
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PIKfyve
PtdIns(3) 5-kinase
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type III PIP kinase
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phosphatidylinositol 3-phosphate 5-kinase
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
phospho-group transfer
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SYSTEMATIC NAME
IUBMB Comments
ATP:1-phosphatidyl-1D-myo-inositol-3-phosphate 5-phosphotransferase
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CAS REGISTRY NUMBER
COMMENTARY
190606-24-7
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SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
ATP + 1-phosphatidyl-1D-myo-inositol 3-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 3,5-bisphosphate
additional information
?
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PIKfyve participates in the SGK1-dependent regulation of the Na+, glucose cotransporter SGLT1 (SLC5A1)
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?
ATP + 1-phosphatidyl-1D-myo-inositol 3-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 3,5-bisphosphate
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?
ATP + 1-phosphatidyl-1D-myo-inositol 3-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 3,5-bisphosphate
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?
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
ATP + 1-phosphatidyl-1D-myo-inositol 3-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 3,5-bisphosphate
additional information
?
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PIKfyve participates in the SGK1-dependent regulation of the Na+, glucose cotransporter SGLT1 (SLC5A1)
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?
ATP + 1-phosphatidyl-1D-myo-inositol 3-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 3,5-bisphosphate
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?
ATP + 1-phosphatidyl-1D-myo-inositol 3-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 3,5-bisphosphate
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COFACTOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
apilimod
an inhibitor of the main endosomal phosphatidylinositol-3-phosphate/phosphatidylinositol 5-kinase, PIKfyve, and potent inhibitor of SARS-CoV-2 strain 2019-nCoV/USA-WA1/2020. The compound prevents cytoplasmic entry of MeGFP-tagged vesicular stomatitis virus (VSV)-ebolavirus (EBOV) construct VSV-MeGFP-ZEBOV, inhibition of VSV mutant entry, overview. The virus particles are able to enter functional endosomes in presence of apilimod; HY-14644, apilimod inhibits enzyme PIKfyve and infection of SARS-CoV-2 virus. The IC50 of apilimod in experiments with authentic virus is remarkably similar to (or even more potent than) that obtained with chimeric VSV-SARS-CoV-2
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vacuolin-1
an inhibitor of the main endosomal phosphatidylinositol-3-phosphate/phosphatidylinositol 5-kinase, PIKfyve. The compound prevents cytoplasmic entry of MeGFP-tagged vesicular stomatitis virus (VSV)-ebolavirus (EBOV) construct VSV-MeGFP-ZEBOV, inhibition of VSV mutant entry, overview; vacuolin-1 inhibits enzyme PIKfyve
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ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
additional information
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enzyme synthesis is stimulated by a hyperosmotic shock
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ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
localizes mainly to early endosomes. PIKfyve is distributed in microdomains
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PIKfyve is predominantly associated with the early endosome, from where it regulates retrograde membrane trafficking to the trans-Golgi-network
cytosolic face of endosomal membranes as part of a ternary complex with the PI(3,5)P2 5-phosphatase Sac3 and ArPIKfyve
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
malfunction
the intracellular trafficking of pathogens, Zaire EBOV GP (VSV-MeGFPZEBOV) and SARS-CoV-2 S Wuhan-Hu-1 strain (VSV-eGFP-SARS-CoV-2), is elicited by inhibition of PIKfyve kinase via apilimod and vacuolin-1, small-molecule inhibitors of the main endosomal phosphatidylinositol-3-phosphate/phosphatidylinositol 5-kinase, PIKfyve
physiological function
analysis of the intracellular trafficking of pathogens elicited by inhibition of PIKfyve kinase
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable).
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable). FYV1_HUMAN
2098
0
237136
Swiss-Prot
other Location (Reliability: 1)
V9HWG4_HUMAN
2098
0
237108
TrEMBL
other Location (Reliability: 1)
PDB
SCOP
CATH
UNIPROT
ORGANISM
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
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the PIPkin type III family enzyme consists of 4 typical domains: the FYVE RING Zn-finger domain, the TCP-I/chaperone-like domain, the PIPkin domain, and the cysteine-rich domain, the human enzyme contains additionally a DEP domain
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
drug development
drug development
potential for targeting this kinase in developing small-molecule antivirals against SARS-CoV-2. The infection is fully blocked by bafilomycin A1, which inhibits the vacuolar type H+-ATPase (V-ATPase) acidification activity. Apilimod and vacuolin-1 prevent cytoplasmic entry of VSV-MeGFP-ZEBOV (from Zaire ebolavirus VSV-ZEBOV)
drug development
the enzyme is a potential target for developing small-molecule antivirals against SARS-CoV-2
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Cooke, F.T.
Phosphatidylinositol 3,5-bisphosphate: metabolism and function
Arch. Biochem. Biophys.
407
143-151
2002
Arabidopsis thaliana, Caenorhabditis elegans, Candida albicans, Drosophila melanogaster, Homo sapiens, Mus musculus, Oryza sativa, Schizosaccharomyces pombe, Saccharomyces cerevisiae (P34756)
Shojaiefard, M.; Strutz-Seebohm, N.; Tavare, J.M.; Seebohm, G.; Lang, F.
Regulation of the Na(+), glucose cotransporter by PIKfyve and the serum and glucocorticoid inducible kinase SGK1
Biochem. Biophys. Res. Commun.
359
843-847
2007
Homo sapiens
Cabezas, A.; Pattni, K.; Stenmark, H.
Cloning and subcellular localization of a human phosphatidylinositol 3-phosphate 5-kinase, PIKfyve/Fab1
Gene
371
34-41
2006
Homo sapiens (Q9Y2I7), Homo sapiens
Rutherford, A.C.; Traer, C.; Wassmer, T.; Pattni, K.; Bujny, M.V.; Carlton, J.G.; Stenmark, H.; Cullen, P.J.
The mammalian phosphatidylinositol 3-phosphate 5-kinase (PIKfyve) regulates endosome-to-TGN retrograde transport
J. Cell Sci.
119
3944-3957
2006
Homo sapiens
Kang, Y.L.; Chou, Y.Y.; Rothlauf, P.W.; Liu, Z.; Soh, T.K.; Cureton, D.; Case, J.B.; Chen, R.E.; Diamond, M.S.; Whelan, S.P.J.; Kirchhausen, T.
Inhibition of PIKfyve kinase prevents infection by Zaire ebolavirus and SARS-CoV-2
Proc. Natl. Acad. Sci. USA
117
20803-20813
2020
Homo sapiens (Q9Y2I7)
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