Open Access

ZGDHu‑1 for cancer therapy (Review)

  • Authors:
    • Jinlin Liu
    • Liannv Qiu
    • Jun Xia
    • Sufeng Chen
    • Xiping Yu
    • Yonglie Zhou
  • View Affiliations

  • Published online on: September 28, 2017
  • Pages:6334-6340
  • Copyright: © Liu et al. This is an open access article distributed under the terms of Creative Commons Attribution License.

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N,N'‑di‑(m‑methylphenyl)‑3,6‑dimethyl‑1,4‑dihydro‑1,2,4,5‑tetrazine‑1,4‑dicarboamide (ZGDHu‑1) is a novel tetrazine derivative that was initially designed and produced by Professor W.X. Hu, and which has been reported by our group to exhibit antitumor activity. Accumulating evidence suggests that the anticancer mechanisms of ZGDHu‑1 may be involved indifferent biological activities, particularly in acute myeloid leukemia (AML) cells. At a high concentration, ZGDHu‑1 has been demonstrated to inhibit the proliferation of the leukemia cells by arresting the cell cycle at the G2/M phase, and by inducing cell apoptosis via inducing the accumulation of reactive oxygen species, the translocation of phosphatidylserine across the plasma membrane and the loss of mitochondrial membrane potential. Furthermore, at a low concentration, it was demonstrated to induce the differentiation and degrade the AML1‑eight‑twenty‑one fusion protein in AML cells. Finally, results from a previous study indicate that ZGDHu‑1 is a potential proteasome inhibitor. Overall, our preliminary research suggests that ZGDHu‑1 may be a promising anticancer drug; however, further research is warranted to identify the exact drug target and potential clinical application in leukemia cells or solid tumors. In the present review, the application of ZGDHu‑1 in cancer research, in addition to the specific underlying targets of ZGDHu‑1, are discussed.

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December 2017
Volume 14 Issue 6

Print ISSN: 1792-1074
Online ISSN:1792-1082

2016 Impact Factor: 1.39
Ranked #68/217 Oncology
(total number of cites)

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Copy and paste a formatted citation
Liu, J., Qiu, L., Xia, J., Chen, S., Yu, X., & Zhou, Y. (2017). ZGDHu‑1 for cancer therapy (Review). Oncology Letters, 14, 6334-6340.
Liu, J., Qiu, L., Xia, J., Chen, S., Yu, X., Zhou, Y."ZGDHu‑1 for cancer therapy (Review)". Oncology Letters 14.6 (2017): 6334-6340.
Liu, J., Qiu, L., Xia, J., Chen, S., Yu, X., Zhou, Y."ZGDHu‑1 for cancer therapy (Review)". Oncology Letters 14, no. 6 (2017): 6334-6340.