Journal
EMBO REPORTS
Volume 9, Issue 2, Pages 164-170Publisher
WILEY
DOI: 10.1038/sj.embor.7401155
Keywords
phosphoinositides; PIKfyve; membrane transport; kinase inhibitor
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Funding
- Biotechnology and Biological Sciences Research Council [BB/E001521/1] Funding Source: Medline
- Wellcome Trust Funding Source: Medline
- BBSRC [BB/E001521/1] Funding Source: UKRI
- Biotechnology and Biological Sciences Research Council [BB/E001521/1] Funding Source: researchfish
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Phosphoinositides have crucial roles in cellular controls, many of which have been established through the use of small-molecule inhibitors. Here, we describe YM201636, a potent inhibitor of the mammalian class III phosphatidylinositol phosphate kinase PIKfyve, which synthesizes phosphatidylinositol 3,5-bisphosphate. Acute treatment of cells with YM201636 shows that the PIKfyve pathway is involved in the sorting of endosomal transport, with inhibition leading to the accumulation of a late endosomal compartment and blockade of retroviral exit. Inhibitor specificity is shown by the use of short interfering RNA against the target, as well as by rescue with the drug-resistant yeast orthologue Fab1. We concluded that the phosphatidylinositol 3,5-bisphosphate pathway is integral to endosome formation, determining morphology and cargo flux.
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