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Research progress of LSD1-based dual-target agents for cancer therapy
1School of Pharmacy, Xinxiang University, Xinxiang 453003, China.
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.
Insights
Lysine-specific demethylase 1 (LSD1) is a promising cancer target. New dual-target agents aim to overcome resistance and toxicity issues associated with current LSD1 inhibitors for improved cancer therapy.
Area of Science:
- Oncology
- Molecular Biology
- Medicinal Chemistry
Background:
- Lysine-specific demethylase 1 (LSD1) is overexpressed in various cancers, impacting cell growth, invasion, migration, immune escape, and angiogenesis.
- LSD1 plays critical roles in gene regulation and transcription, making it a significant target for anticancer drug development.
Purpose of the Study:
- To review the theoretical basis for designing novel LSD1-based dual-target agents.
- To summarize the potential applications of these agents in cancer treatment.
Main Methods:
- Discussion of the rationale behind dual-target strategies involving LSD1.
- Review of existing literature on LSD1 inhibitors and dual-target agents.
Main Results:
- Current LSD1 inhibitors face challenges due to resistance, low selectivity, limited efficacy, and high toxicity.
- LSD1 inhibitors demonstrate synergistic effects with other antitumor drugs, driving the development of new agents.
Conclusions:
- Developing new-generation LSD1-based dual-target agents is crucial to overcome therapeutic limitations.
- These novel agents hold promise for enhanced efficacy and reduced toxicity in cancer treatment.
