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Issue 2, 2011
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Chemical proteomics reveals bolinaquinone as a clathrin-mediated endocytosis inhibitor

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Abstract

The emerging field of mass spectrometry-based chemical proteomics provides a powerful instrument in the target discovery of bioactive small-molecules, such as drugs or natural products. The identification of their macromolecular targets is required for a comprehensive understanding of their bio-pharmacological role and for unraveling their mechanism of action. We report the application of a chemical proteomics approach to the analysis of the cellular interactome of the marine metabolite bolinaquinone (BLQ). BLQ was linked to an opportune α,ω-diamino polyethylene glycol chain and then immobilized on a matrix support. The modified beads were then used as a bait for fishing the potential partners of BLQ in a THP-1 macrophage cell lysate. Surprisingly, we identified clathrin, a protein involved in the cell internalization of proteins, viruses and other biologically relevant macromolecules, as a specific and major BLQ partner. In addition, we verified the biochemical role of BLQ testing its ability to inhibit the clathrin-mediated endocytosis of albumin. This finding indicates BLQ as a new biotechnological tool for cell endocytosis studies and paves the way to further investigation on its potential role in modulating internalization process.

Graphical abstract: Chemical proteomics reveals bolinaquinone as a clathrin-mediated endocytosis inhibitor

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Publication details

The article was received on 30 Jul 2010, accepted on 05 Oct 2010 and first published on 08 Nov 2010


Article type: Paper
DOI: 10.1039/C0MB00126K
Citation: Mol. BioSyst., 2011,7, 480-485
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    Chemical proteomics reveals bolinaquinone as a clathrin-mediated endocytosis inhibitor

    L. Margarucci, M. C. Monti, B. Fontanella, R. Riccio and A. Casapullo, Mol. BioSyst., 2011, 7, 480
    DOI: 10.1039/C0MB00126K

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