Target intelligence / Profile preview

Phosphoinositide kinase, FYVE-type zinc finger containing (PIKFYVE)

Target
PIKFYVE
Molecular classification
Enzyme, Lipid Kinase
01

Overview

PIKfyve is a lipid kinase that phosphorylates phosphatidylinositol 3-phosphate (PtdIns3P) to generate phosphatidylinositol 3,5-bisphosphate [PI(3,5)P₂]. It also plays a role in the production of phosphatidylinositol 5-phosphate [PI(5)P]. These phosphoinositides are critical regulators of endosome–lysosome–autophagy signaling pathways and vesicular trafficking. PIKfyve dysfunction is linked to defects in vesicle trafficking/endolysosomal system and is implicated in neurodegenerative disorders, several cancers, and viral entry.

Other names
PIP5K3FYV1
02

Mechanism of action

Inhibition of PIKfyve kinase activity, disrupting TLR signaling and endolysosomal pathways.

03

Biological functions

Endolysosomal trafficking/fissionIon homeostasisAutophagy regulationVesicular trafficking
04

Disease associations

NeurodegenerationCancerViral infection
05

Safety considerations

Cytoplasmic vacuolation due to defective lysosome fission/homeostasis
06

Interacting drugs

Apilimod

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