Vacuolin-1 inhibits autophagy by impairing lysosomal maturation via PIKfyve inhibition - PubMed (original) (raw)

. 2016 Jun;590(11):1576-85.

doi: 10.1002/1873-3468.12195. Epub 2016 May 13.

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Vacuolin-1 inhibits autophagy by impairing lysosomal maturation via PIKfyve inhibition

Osamu Sano et al. FEBS Lett. 2016 Jun.

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Abstract

Lysosomal protein degradation via autophagy strictly regulates cellular protein homoeostasis. Herein we performed high-content screening to identify compounds that inhibit autophagy pathways. We obtained 11 hit compounds and performed cluster analysis using cellular morphological information. Vacuolin-1, which induces the formation of giant vacuoles and is a target unknown compound, clustered with the known PIKfyve inhibitor YM201636. We further confirmed that vacuolin-1 is a potent PIKfyve inhibitor, and we finally concluded that PIKfyve inhibitors are novel chemical tools for regulating autophagy.

Keywords: PIKfyve; autophagy; vacuolin-1.

© 2016 Federation of European Biochemical Societies.

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