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Combination Therapy and Dual-Target Inhibitors Based on LSD1: New Emerging Tools in Cancer Therapy

Liang Shen1, Bo Wang1, Shao-Peng Wang1

  • 1Key Lab of Advanced Drug Preparation Technologies, Ministry of Education of China; State Key Laboratory of Esophageal Cancer Prevention & Treatment; Key Laboratory of Henan Province for Drug Quality and Evaluation; Institute of Drug Discovery and Development; School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou 450001, Henan, China.

Journal of Medicinal Chemistry
|January 12, 2024
PubMed

Insights

Lysine specific demethylase 1 (LSD1) inhibitors show promise in cancer therapy, with many entering clinical trials. Combining LSD1 inhibitors with other agents or developing multitarget inhibitors may enhance anti-cancer efficacy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Lysine specific demethylase 1 (LSD1) is a transcriptional modulator overexpressed in many cancers, disrupting normal gene expression.
  • LSD1's role in cancer necessitates the development of targeted therapeutic strategies.

Purpose of the Study:

  • To provide a comprehensive overview of LSD1 inhibitors in cancer therapy.
  • To explore the combination of LSD1 inhibitors with other antitumor agents.
  • To discuss LSD1 multitarget inhibitors and future research directions.

Main Methods:

  • Review of published literature on LSD1 inhibitors and their clinical applications.
  • Analysis of existing and emerging LSD1-targeted therapies.
  • Discussion of combination strategies and multitargeting approaches.

Main Results:

  • Numerous irreversible and reversible LSD1 inhibitors have been developed, with several in clinical trials.
  • Combination therapies involving LSD1 inhibitors show enhanced efficacy.
  • Dual LSD1/histone deacetylase (HDAC) inhibitors represent a multitargeting strategy.

Conclusions:

  • LSD1 inhibitors are a promising class of anticancer agents.
  • Combination therapies and multitargeting strategies hold significant potential for improving cancer treatment outcomes.
  • Further research into LSD1-targeted agents is warranted.

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