1. Academic Validation
  2. Research progress of LSD1-based dual-target agents for cancer therapy

Research progress of LSD1-based dual-target agents for cancer therapy

  • Bioorg Med Chem. 2024 Mar 1:101:117651. doi: 10.1016/j.bmc.2024.117651.
Xiaojuan Yang 1
Affiliations

Affiliation

  • 1 School of Pharmacy, Xinxiang University, Xinxiang 453003, China. Electronic address: yxj3188@163.com.
Abstract

Lysine-specific demethylase 1 (LSD1) is a histone lysine demethylase that is significantly overexpressed or dysregulated in different cancers and plays important roles in cell growth, invasion, migration, immune escape, angiogenesis, gene regulation, and transcription. Therefore, it is a superb target for the discovery of novel antitumor agents. However, because of their innate and acquired resistance and low selectivity, LSD1 inhibitors are associated with limited therapeutic efficacy and high toxicity. Furthermore, LSD1 inhibitors synergistically improve the efficacy of additional antitumor drugs, which encourages numerous medicinal chemists to innovate and develop new-generation LSD1-based dual-target agents. This review discusses the theoretical foundation of the design of LSD1-based dual-target agents and summarizes their possible applications in treating cancers.

Keywords

Cancer therapy; Dual-target agents; LSD1; Synergistic effect.

Figures
Products