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

20 Citations (Scopus)

Abstract

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
Volume14
Issue number12
DOIs
Publication statusPublished - 2019 Dec 20
Externally publishedYes

Bibliographical note

Funding Information:
Funding was provided by National Natural Science Foundation of China (81803389, 21602079, 21877050), Science and Technology Program of Guangdong Province (2017A050506028, 2019B151502025), Science and Technology Program of Guangzhou (201704030060, 201805010007), China Postdoctoral Science Foundation (No.2017M622923), and the Ph.D. Start-up Fund of Natural Science Foundation of Guangdong Province, China (NO. 2018A030310651). We thank S. Q. Yao (NUS, Singapore) for the invaluable suggestions and support on this work.

Funding Information:
Funding was provided by National Natural Science Foundation of China (81803389, 21602079, 21877050), Science and Technology Program of Guangdong Province (2017A050506028, 2019B151502025), Science and Technology Program of Guangzhou (201704030060, 201805010007) China Postdoctoral Science Foundation (No.2017M622923), and the Ph.D. Start-up Fund of Natural Science Foundation of Guangdong Province China (NO. 2018A030310651). We thank S. Q. Yao (NUS, Singapore) for the invaluable suggestions and support on this work.

Publisher Copyright:
Copyright © 2019 American Chemical Society.

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine

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