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Literature summary extracted from

  • 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 (2020), Proc. Natl. Acad. Sci. USA, 117, 20803-20813 .
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
2.7.1.150 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) Homo sapiens
2.7.1.150 drug development the enzyme is a potential target for developing small-molecule antivirals against SARS-CoV-2 Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.150 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 Homo sapiens
2.7.1.150 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 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.7.1.150 endosome membrane
-
 Homo sapiens 10008
-
2.7.1.150 endosome membrane cytosolic face of endosomal membranes as part of a ternary complex with the PI(3,5)P2 5-phosphatase Sac3 and ArPIKfyve Homo sapiens 10008
-
2.7.1.150 vacuolar membrane
-
 Homo sapiens 5774
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.1.150 Mg2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.1.150 ATP + 1-phosphatidyl-1D-myo-inositol 3-phosphate Homo sapiens
-
 ADP + 1-phosphatidyl-1D-myo-inositol 3,5-bisphosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.150 Homo sapiens Q9Y2I7
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.1.150 astroglial cell astroglial SVG-A derived cells Homo sapiens
-
2.7.1.150 SVG-A cell astroglial-derived cells Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.1.150 ATP + 1-phosphatidyl-1D-myo-inositol 3-phosphate
-
 Homo sapiens ADP + 1-phosphatidyl-1D-myo-inositol 3,5-bisphosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.1.150 class III lipid kinase
-
 Homo sapiens
2.7.1.150 phosphatidylinositol-3-phosphate/phosphatidylinositol 5-kinase
-
 Homo sapiens
2.7.1.150 PI-3P-5-kinase
-
 Homo sapiens
2.7.1.150 PIKfyve
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.1.150 ATP
-
 Homo sapiens

General Information

EC Number General Information Comment Organism
2.7.1.150 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 Homo sapiens
2.7.1.150 physiological function analysis of the intracellular trafficking of pathogens elicited by inhibition of PIKfyve kinase Homo sapiens