ABSTRACT

Introduction

Lysine-specific demethylase 1 (LSD1), which belongs to the demethylase of non-histone proteins, is believed to promote cancer cell proliferation and metastasis by modifying histones. LSD1 dysfunction may play a key role in a variety of cancers, such as acute myeloid leukemia and non-small cell lung cancer, indicating that LSD1 is a promising epigenetic target for cancer therapy. Many different types of small molecule LSD1 inhibitors have been developed and shown to inhibit tumor cell proliferation, invasion, and migration, providing a new treatment strategy for solid tumors.

Areas covered

This review summarizes the progress of LSD1 inhibitor research in the last four years, including selected new patents and article publications, as well as the therapeutic potential of these compounds.

Expert opinion

Natural products offer a promising prospect for developing novel potent LSD1 inhibitors, as structural design and activity of irreversible and reversible inhibitors have been continuously optimized since the discovery of the LSD1 target in 2004. The use of ‘microtubule-binding agents’ and ‘dual-agent combination’ has recently become a new anticancer technique, reducing the resistance and adverse reactions of traditional drugs. Several microtubule-binding drugs have been used successfully in clinical practice, providing structural scaffolds and new ideas for the development of safer drugs.

中文翻译：

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用于抗癌治疗的 LSD1 抑制剂：专利审查（2017 年至今）

摘要

介绍

赖氨酸特异性去甲基化酶1（LSD1）属于非组蛋白的去甲基化酶，被认为通过修饰组蛋白促进癌细胞增殖和转移。LSD1功能障碍可能在多种癌症中发挥关键作用，例如急性髓细胞白血病和非小细胞肺癌，表明LSD1是癌症治疗的有希望的表观遗传靶点。许多不同类型的小分子LSD1抑制剂已被开发出来，并显示出抑制肿瘤细胞增殖、侵袭和迁移的作用，为实体瘤提供了一种新的治疗策略。

涵盖的领域

这篇综述总结了近四年来LSD1抑制剂的研究进展，包括选定的新专利和文章发表，以及这些化合物的治疗潜力。

专家意见

天然产物为开发新型强效 LSD1 抑制剂提供了广阔的前景，因为自 2004 年发现 LSD1 靶标以来，不可逆和可逆抑制剂的结构设计和活性一直在不断优化。“微管结合剂”和“双重抑制剂”的使用药物组合'最近成为一种新的抗癌技术，减少了传统药物的耐药性和不良反应。几种微管结合药物已成功应用于临床，为开发更安全的药物提供了结构支架和新思路。