Journal of Enzyme Inhibition and Medicinal Chemistry (Jan 2020)

An overview on natural farnesyltransferase inhibitors for efficient cancer therapy

  • Xiaohan Dai,
  • Yingni Sun,
  • Ting Zhang,
  • Yongfei Ming,
  • Gao Hongwei

DOI
https://doi.org/10.1080/14756366.2020.1732366
Journal volume & issue
Vol. 35, no. 1
pp. 1027 – 1044

Abstract

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As one of the world’s five terminally ills, tumours can cause important genetic dysfunction. However, some current medicines for tumours usually have strong toxic side effects and are prone to drug resistance. Studies have found that farnesyltransferase inhibitors (FTIs) extracted from natural materials have a good inhibiting ability on tumours with fewer side effects. This article describes several FTIs extracted from natural materials and clarifies the current research progress, which provides a new choice for the treatment of tumours. Executive summary Farnesyltransferase (FTase) When Ras gene is activated, it becomes an oncogene with oncogenic activity. Ras protein plays a crucial role in cancer cells. FTase is the first step to activate Ras protein. FTIs not only have anti-tumour effects, but also makes great contribution to the treatment of plasmodium falciparum, parasitic diseases and progeria. There are still some problems with FTIs, but natural products FTIs are worthy of further research as a new class of low-toxic, safe and effective anticancer drugs. Summarised natural product-derived FTase inhibitors This review summarised several FTIs extracted from natural materials and clarifies their anti-tumour activity (IC50 value) and structure, providing a reference for further research on tumour therapy.

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