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Lysine-Specific Demethylase 1 Promises to Be a Novel Target in Cancer Drug Resistance: Therapeutic Implications

Fei-Fei Yang1, Xue-Li Xu1, Ting Hu1

  • 1State Key Laboratory of Esophageal Cancer Prevention and Treatment, Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China, School of Pharmaceutical Science and Institute of Pharmaceutical Science, Zhengzhou University, Zhengzhou, Henan 450001, China.

Journal of Medicinal Chemistry
|April 4, 2023
PubMed

Insights

Lysine-specific demethylase 1 (LSD1) plays a key role in cancer drug resistance. Targeting LSD1 may restore sensitivity to cancer therapies like immune checkpoint inhibitors (ICIs).

Area of Science:

  • Oncology
  • Molecular Biology
  • Epigenetics

Background:

  • Cancer therapies like chemotherapy and immunotherapy face challenges due to drug resistance.
  • Lysine-specific demethylase 1 (LSD1) is an epigenetic regulator involved in tumor progression and metastasis.
  • LSD1 influences tumor cell invasion, apoptosis, and immune escape, contributing to tumorigenesis.

Purpose of the Study:

  • To review recent findings on Lysine-specific demethylase 1 (LSD1) biology in cancer.
  • To explore LSD1's role in the development and progression of cancer drug resistance.
  • To summarize LSD1 inhibitors and their potential to overcome drug resistance.

Main Methods:

  • Literature review of recent studies on LSD1.
  • Analysis of LSD1's involvement in cancer drug resistance mechanisms.
  • Summary of existing and potential LSD1 inhibitors.

Main Results:

  • LSD1 ablation can resensitize tumor cells to anticarcinogens, including immune checkpoint inhibitors (ICIs).
  • LSD1 regulates multiple upstream and downstream pathways affecting drug sensitivity.
  • Several LSD1 inhibitors show potential in reversing or resensitizing tumors to therapy.

Conclusions:

  • LSD1 is a critical factor in cancer drug resistance.
  • Targeting LSD1, potentially in combination with other agents, offers a promising strategy to overcome treatment resistance.
  • Further research into LSD1 inhibitors could lead to novel cancer therapeutics.

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