Literature summary for 2.7.1.150 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 .

Search for more literature for 2.7.1.150

Application

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

Inhibitors

Inhibitors	Comment	Organism	Structure
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
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

Localization	Comment	Organism	GeneOntology No.	Textmining
endosome membrane	-	Homo sapiens	10008	-
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	-
vacuolar membrane	-	Homo sapiens	5774	-

Metals/Ions

Metals/Ions	Comment	Organism	Structure
Mg2+	required	Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	Q9Y2I7	-	-

Source Tissue

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

Substrates and Products (Substrate)

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

Synonyms

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

Cofactor

Cofactor	Comment	Organism	Structure
ATP	-	Homo sapiens

General Information

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

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Release 2023.1 (January 2023)