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  3. High-throughput screening suggests glutathione synthetase as an anti-tumor target of polydatin using human proteome chip

High-throughput screening suggests glutathione synthetase as an anti-tumor target of polydatin using human proteome chip

  • Int J Biol Macromol. 2020 Oct 15:161:1230-1239. doi: 10.1016/j.ijbiomac.2020.06.061.
Peng Chen 1,  Lei Wang 2,  Shutao Sun 3,  Qingbing Zhou 4,  Zehua Zeng 2,  Mingliang Hu 5,  Muhammad Hussain 2,  Cheng Lu 6,  Hongwu Du 7
Affiliations

Affiliations

  • 1 Beijing Key Laboratory of Traditional Chinese Medicine Basic Research on Prevention and Treatment for Major Diseases, Experimental Research Center, China Academy of Chinese Medical Sciences, Beijing, China. Electronic address: [email protected].
  • 2 School of Chemistry and Biological Engineering, University of Science and Technology Beijing, Beijing, China.
  • 3 Public Technology Service Center, Institute of Microbiology, Chinese Academy of Sciences, Beijing, China.
  • 4 Institute of Geriatric Medicine, Xiyuan Hospital, China Academy of Chinese Medical Sciences, Beijing, China.
  • 5 Key Laboratory for Research on Active Ingredients in Natural Medicine of Jiangxi Province, Yichun University, Yichun, China; Institute of Basic Research in Clinical Medicine, China Academy of Chinese Medical Sciences, Beijing, China.
  • 6 Institute of Basic Research in Clinical Medicine, China Academy of Chinese Medical Sciences, Beijing, China. Electronic address: [email protected].
  • 7 School of Chemistry and Biological Engineering, University of Science and Technology Beijing, Beijing, China. Electronic address: [email protected].
PMID: 32544581 DOI: 10.1016/j.ijbiomac.2020.06.061
Abstract

Polydatin (PD) is a bio-active ingredient with known anti-tumor effects. However, its specific protein targets yet have not been systematically screened, and the molecular anti-tumor mechanism is still unclear. Here, proteomic-chip was efficiently used to screen potential targets of PD. First, we investigated through animal experiment and proteomics studies, and found that polydatin play an important role in tumor cells. Then, the red-green fluorescent of polydatin was compared comprehensively to screen its targets on chip, followed by bioinformatics analysis. Glutathione synthetase (GSS) was selected as candidate research target. After a series of molecular biological experiments GSS was confirmed a target protein for PD in vitro. Moreover, we also found that PD can significantly inhibit the activity of GSS in vitro and live cells. Our findings reveal that PD could be a selective small-molecule GSS Enzyme activity inhibitor and GSS could be a potential therapeutic target in Cancer.

Keywords

Cancer treatment; Drug targets; Glutathione synthetase; Proteomic chip.

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