Recent researches for dual Aurora target inhibitors in antitumor field

Eur J Med Chem. 2020 Oct 1:203:112498. doi: 10.1016/j.ejmech.2020.112498. Epub 2020 Jun 26.

Abstract

Non-infectious and chronic diseases such as malignant tumors are now one of the main causes of human death. Its occurrence is a multi-factor, multi-step complex process with biological characteristics such as cell differentiation, abnormal proliferation, uncontrolled growth, and metastasis. It has been found that a variety of human malignant tumors are accompanied by over-expression and proliferation of Aurora kinase, which causes abnormalities in the mitotic process and is related to the instability of the genome that causes tumors. Therefore, the use of Aurora kinase inhibitors to target tumors is becoming a research hotspot. However, in cancer, because of the complexity of signal transduction system and the participation of different proteins and enzymes, the anticancer effect of selective single-target drugs is limited. After inhibiting one pathway, signal molecules can be conducted through other pathways, resulting in poor therapeutic effect of single-target drug treatment. Multi-target drugs can solve this problem very well. It can regulate the various links that cause disease at the same time without completely eliminating the relationship between the signal transmission systems, and it is not easy to cause drug resistance. Currently, studies have shown that Aurora dual-target inhibitors generated with the co-inhibition of Aurora and another target (such as CDK, PLK, JAK2, etc.) have better therapeutic effects on tumors. In this paper, we reviewed the studies of dual Aurora inhibitors that have been discovered in recent years.

Keywords: Anti-tumor; Aurora kinase; Dual inhibitor.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Aurora Kinases / antagonists & inhibitors*
  • Drug Discovery*
  • Humans
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / pharmacology*

Substances

  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • Aurora Kinases