TitleActivity- based protein profiling reveals GSTO1 as the covalent target of piperlongumine and a promising target for combination therapy for cancer
AuthorsLi, Li
Zhao, Yue
Cao, Ran
Li, Lin
Cai, Gaihong
Li, Jiaojiao
Qi, Xiangbing
Chen, She
Zhang, Zhiyuan
AffiliationNIBS, 7 Sci Pk Rd,ZGC Life Sci Pk, Beijing, Peoples R China
China Agr Univ, Coll Biol Sci, Beijing 100193, Peoples R China
Peking Univ, Sch Life Sci, 5 Yiheyuan Rd, Beijing, Peoples R China
Issue Date2019
AbstractThrough 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.
Appears in Collections:生命科学学院

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