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Issue 21, 2019
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Development of ergosterol peroxide probes for cellular localisation studies

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Abstract

Ergosterol peroxide selectively exhibits biological activity against a wide range of diseases; however, its mode of action remains unknown. Here, we present an efficient synthesis of ergosterol peroxide chemical probes for in vitro anticancer evaluation, live cell studies and proteomic profiling. Ergosterol peroxide analogues show promising anti-proliferation activity against triple negative breast cancer cellular models, revealing information on the structure–activity relationship of this natural product in order to develop superior analogues. The combined cellular studies demonstrate that ergosterol peroxide is distributed across the cytosol with significant accumulation in the endoplasmic reticulum (ER). These chemical probes support our efforts towards uncovering the potential target(s) of ergosterol peroxide against triple negative breast cancer cell lines.

Graphical abstract: Development of ergosterol peroxide probes for cellular localisation studies

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Publication details

The article was received on 19 Jan 2019, accepted on 14 Mar 2019 and first published on 26 Apr 2019


Article type: Communication
DOI: 10.1039/C9OB00145J
Org. Biomol. Chem., 2019,17, 5223-5229
  • Open access: Creative Commons BY-NC license
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    Development of ergosterol peroxide probes for cellular localisation studies

    T. Ling, W. H. Lang, M. M. Martinez-Montemayor and F. Rivas, Org. Biomol. Chem., 2019, 17, 5223
    DOI: 10.1039/C9OB00145J

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