Affinity-Based Protein Profiling Reveals Cellular Targets of Photoreactive Anticancer Inhibitors

Nan Ma, Zhi Min Zhang, Jun Seok Lee, Ke Cheng, Ligen Lin, Dong Mei Zhang, Piliang Hao, Ke Ding, Wen Cai Ye, Zhengqiu Li

Research output: Contribution to journalArticlepeer-review

17 Citations (Scopus)


Affinity-based protein profiling has proven to be a powerful method in target identification of bioactive molecules. Here, this technology was applied in two photoreactive anticancer inhibitors, arenobufagin and HM30181. Using UV irradiation, these photoreactive reagents can covalently cross-link to target proteins, leading to a covalent binding with target proteins. Moreover, the cellular on/off targets of these two molecules, including ATP1A1, MDR1, PARP1, DDX5, NOP2, RAB6A, and ERGIC1 were first identified by affinity-based protein profiling and bioimaging approaches. The protein hit, PARP1, was further validated to be involved in the function of the anticancer effects.

Original languageEnglish
Pages (from-to)2546-2552
Number of pages7
JournalACS Chemical Biology
Issue number12
Publication statusPublished - 2019 Dec 20
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine


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