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  3. A novel L-shaped ortho-quinone analog as PLK1 inhibitor blocks prostate cancer cells in G2 phase

A novel L-shaped ortho-quinone analog as PLK1 inhibitor blocks prostate cancer cells in G2 phase

  • Biochem Pharmacol. 2023 Dec 3:219:115960. doi: 10.1016/j.bcp.2023.115960.
Shaowei Zhang 1,  Jia Yu 2,  Xin Tan 2,  Sha Cheng 2,  Hanfei Liu 2,  Zhiyao Li 2,  Shinan Wei 2,  Weidong Pan 3,  Heng Luo 4
Affiliations

Affiliations

  • 1 State Key Laboratory for Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550014, China; Natural Products Research Center of Guizhou Province, Guiyang 550014, Guizhou Province, China; School of Pharmaceutical Sciences, Guizhou Medical University, Guiyang 550025, China.
  • 2 State Key Laboratory for Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550014, China; Natural Products Research Center of Guizhou Province, Guiyang 550014, Guizhou Province, China.
  • 3 State Key Laboratory for Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550014, China; Natural Products Research Center of Guizhou Province, Guiyang 550014, Guizhou Province, China. Electronic address: weidongpan@gzcnp.cn.
  • 4 State Key Laboratory for Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550014, China; Natural Products Research Center of Guizhou Province, Guiyang 550014, Guizhou Province, China. Electronic address: luo_heng@gmc.edu.cn.
PMID: 38049008 DOI: 10.1016/j.bcp.2023.115960
Abstract

Prostate Cancer is the most common malignant tumor among men worldwide. Currently, the main treatments are radical prostatectomy, radiotherapy, chemotherapy, and endocrine therapy. However, most of them are poorly effective and induce side effects. Polo-like kinase 1 (PLK1) regulates cell cycle and mitosis. Its inhibitor BI2536 promotes the therapeutic effect of nilotinib in chronic myeloid leukemia, enhances the sensitivity of neural tube cell tumors to radiation therapy and PLK1 silencing enhances the sensitivity of squamous cell carcinoma to cisplatin. Therefore, the aim of this study was to evaluate the effect of the PLK1 Inhibitor L-shaped ortho-quinone analog TE6 on prostate Cancer. In vitro on prostate Cancer cells showed that TE6 inhibited PLK1 protein expression and consequently cell proliferation by blocking the cell cycle at G2 phase. In vivo on a subcutaneous tumor model in nude mice confirmed that TE6 effectively inhibited tumor growth in nude mice, inhibited PLK1 expression and regulated the expression of cell cycle proteins such as p21, p53, CDK1, Cdc25C, and cyclinB1. Thus, PLK1 was identified as the target protein of TE6, these results reveal the critical role of PLK1 in the growth and survival of prostate Cancer and point out the ability of TE6 on targeting PLK1, being a potential drug for prostate Cancer therapy.

Keywords

Cell cycle; Inhibitor; L-shaped ortho-quinone analog; PLK1; Prostate cancer; Targets.

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