赖氨酸特异性去甲基酶 1 抑制剂更新：专利审查（2016-2020 年）。
An Update of Lysine Specific Demethylase 1 Inhibitor: A Patent Review (2016-2020).
机构信息
Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education of China, Key Laboratory of Henan Province for Drug Quality and Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, Henan, 450001, P.R. China.
State Key Laboratory of Esophageal Cancer Prevention & Treatment, Zhengzhou University, Zhengzhou, Henan, 450052, P.R. China.
出版信息
Recent Pat Anticancer Drug Discov. 2022;17(1):9-25. doi: 10.2174/1574892816666210728125224.
BACKGROUND
As a FAD (Flavin Adenine Dinucleotide) - dependent histone demethylase discovered in 2004, LSD1 (lysine-specific demethylase 1) was reported to be overexpressed in diverse tumors, regulating target genes transcription associated with cancer development. Hence, LSD1 targeted inhibitors may represent a new insight in anticancer drug discovery. For these reasons, researchers in both the pharmaceutical industry and academia have been actively pursuing LSD1 inhibitors in the quest for new anti-cancer drugs.
OBJECTIVES
This review summaries patents about LSD1 inhibitors in recent 5 years in the hope of providing a reference for LSD1 researchers to develop new modulators of LSD1 with higher potency and fewer adverse effects.
METHODS
This review collects LSD1 inhibitors disclosed in patents since 2016. The primary ways of patent searching are Espacenet®, Google Patents, and CNKI.
RESULTS
This review covers dozens of patents related to LSD1 inhibitors in recent five years. The compound structures are mainly divided into TCP (Tranylcypromine) derivatives, imidazole derivatives, pyrimidine derivatives, and other natural products and peptides. Meanwhile, the compounds that have entered the clinical phase are also described.
CONCLUSION
Most of the compounds in these patents have been subjected to activity analysis with LSD1 and multi-cell lines, showing good antitumor activity and . These patents exhibited the structural diversity of LSD1 inhibitors and the potential of natural products as novel LSD1 inhibitors.
背景
LSD1（赖氨酸特异性去甲基化酶 1）作为 2004 年发现的一种依赖黄素腺嘌呤二核苷酸（FAD）的组蛋白去甲基化酶，据报道在多种肿瘤中过表达，调节与癌症发展相关的靶基因转录。因此，LSD1 靶向抑制剂可能代表了抗癌药物发现的新视角。出于这些原因，制药行业和学术界的研究人员一直在积极寻求 LSD1 抑制剂，以寻找新的抗癌药物。
目的
本综述总结了近 5 年来 LSD1 抑制剂的专利情况，希望为 LSD1 研究人员开发具有更高效力和更少不良反应的 LSD1 新型调节剂提供参考。
方法
本综述收集了自 2016 年以来专利中公开的 LSD1 抑制剂。专利检索的主要途径是 Espacenet®、Google Patents 和 CNKI。
结果
本综述涵盖了近五年与 LSD1 抑制剂相关的数十项专利。化合物结构主要分为 TCP（曲马多）衍生物、咪唑衍生物、嘧啶衍生物和其他天然产物和肽。同时，还描述了已进入临床阶段的化合物。
结论
这些专利中的大多数化合物都已经过 LSD1 和多种细胞系的活性分析，显示出良好的抗肿瘤活性。这些专利展示了 LSD1 抑制剂的结构多样性和天然产物作为新型 LSD1 抑制剂的潜力。
Zotero 插件