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Issue 30, 2019
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Activity-based protein profiling reveals GSTO1 as the covalent target of piperlongumine and a promising target for combination therapy for cancer

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Abstract

Through systematic target identification for piperlongumine, a cancer-selective killing molecule, we identified GSTO1 as its major covalent target for cancer cell death induction. We also reveal that GSTO1 inhibition is a promising combination strategy with other anti-cancer agents by drug combination screening in which piperlongumine exhibits broad-spectrum synergistic effects with a large proportion of the tested anti-cancer agents, especially with PI3K/Akt/mTOR pathway inhibitors.

Graphical abstract: Activity-based protein profiling reveals GSTO1 as the covalent target of piperlongumine and a promising target for combination therapy for cancer

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Publication details

The article was received on 31 Jan 2019, accepted on 20 Mar 2019 and first published on 27 Mar 2019


Article type: Communication
DOI: 10.1039/C9CC00917E
Chem. Commun., 2019,55, 4407-4410

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    Activity-based protein profiling reveals GSTO1 as the covalent target of piperlongumine and a promising target for combination therapy for cancer

    L. Li, Y. Zhao, R. Cao, L. Li, G. Cai, J. Li, X. Qi, S. Chen and Z. Zhang, Chem. Commun., 2019, 55, 4407
    DOI: 10.1039/C9CC00917E

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