Molecules (Sep 2022)

Biosynthesis of DNA-Alkylating Antitumor Natural Products

  • Qiu-Yue Nie,
  • Yu Hu,
  • Xian-Feng Hou,
  • Gong-Li Tang

DOI
https://doi.org/10.3390/molecules27196387
Journal volume & issue
Vol. 27, no. 19
p. 6387

Abstract

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DNA-alkylating natural products play an important role in drug development due to their significant antitumor activities. They usually show high affinity with DNA through different mechanisms with the aid of their unique scaffold and highly active functional groups. Therefore, the biosynthesis of these natural products has been extensively studied, especially the construction of their pharmacophores. Meanwhile, their producing strains have evolved corresponding self-resistance strategies to protect themselves. To further promote the functional characterization of their biosynthetic pathways and lay the foundation for the discovery and rational design of DNA alkylating agents, we summarize herein the progress of research into DNA-alkylating antitumor natural products, including their biosynthesis, modes of action, and auto-resistance mechanisms.

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