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Issue 69, 2017
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Competitive affinity-based proteome profiling and imaging to reveal potential cellular targets of betulinic acid

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Abstract

Betulinic acid (BA), a pentacyclic triterpenoid natural product, has received considerable attention owing to the broad spectrum of biological activities such as anti-HIV, anti-inflammatory, and especially, antitumor. Despite numerous studies on the antitumor mechanisms over the past decade, the cellular targets in cancer cells remain obscure. Here, we developed two photoprobes, BA-1/BA-2, by attaching terminal alkyne-containing “minimalist” tetrazole/diazirine photo-crosslinkers (L3 and L7) at the C-3 and C-28 positions of BA, respectively, based on well-established structure–activity relationships. The potential cellular targets were identified via competitive proteome profiling and bioimaging approaches.

Graphical abstract: Competitive affinity-based proteome profiling and imaging to reveal potential cellular targets of betulinic acid

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Publication details

The article was received on 31 May 2017, accepted on 01 Aug 2017 and first published on 07 Aug 2017


Article type: Communication
DOI: 10.1039/C7CC04190J
Citation: Chem. Commun., 2017,53, 9620-9623
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    Competitive affinity-based proteome profiling and imaging to reveal potential cellular targets of betulinic acid

    H. Guo, J. Xu, P. Hao, K. Ding and Z. Li, Chem. Commun., 2017, 53, 9620
    DOI: 10.1039/C7CC04190J

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