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J Am Chem Soc. 2017 Feb 1;139(4):1400-1403. doi: 10.1021/jacs.6b11751. Epub 2017 Jan 23.

Click Quantitative Mass Spectrometry Identifies PIWIL3 as a Mechanistic Target of RNA Interference Activator Enoxacin in Cancer Cells.

Author information

1
Department of Molecular Biosciences, University of Texas at Austin , 2500 Speedway, Austin, Texas 78712, United States.
2
UPR2301, Institut de Chimie des Substances Naturelles , 1 avenue de la Terrasse, 91198 Gif-sur-Yvette Cedex, France.
3
Organic Synthesis and Cell Biology Group, Institut Curie, PSL Research University , 26 rue d'Ulm, 75248 Paris Cedex 05, France.
4
CNRS UMR3666 , 75005 Paris, France.
5
INSERM U1143 , 75005 Paris, France.

Abstract

Enoxacin is a small molecule that stimulates RNA interference (RNAi) and acts as a growth inhibitor selectively in cancer but not in untransformed cells. Here, we used alkenox, a clickable enoxacin surrogate, coupled with quantitative mass spectrometry, to identify PIWIL3 as a mechanistic target of enoxacin. PIWIL3 is an Argonaute protein of the PIWI subfamily that is mainly expressed in the germline and that mediates RNAi through piRNAs. Our results suggest that cancer cells re-express PIWIL3 to repress RNAi through miRNAs and thus open a new opportunity for cancer-specific targeting.

PMID:
28094937
DOI:
10.1021/jacs.6b11751
[Indexed for MEDLINE]

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