Display options
Cite
Zheng YC, Liu YJ, Gao Y, et al. An Update of Lysine Specific Demethylase 1 Inhibitor: A Patent Review (2016-2020). Recent Pat Anticancer Drug Discov. 2021;doi: 10.2174/1574892816666210728125224.
Zheng, Y. C., Liu, Y. J., Gao, Y., Wang, B., & Liu, H. M. (2021). An Update of Lysine Specific Demethylase 1 Inhibitor: A Patent Review (2016-2020). Recent patents on anti-cancer drug discovery, . https://doi.org/10.2174/1574892816666210728125224
Zheng, Yi-Chao, et al. "An Update of Lysine Specific Demethylase 1 Inhibitor: A Patent Review (2016-2020)." Recent patents on anti-cancer drug discovery vol. (2021). doi: https://doi.org/10.2174/1574892816666210728125224
Zheng YC, Liu YJ, Gao Y, Wang B, Liu HM. An Update of Lysine Specific Demethylase 1 Inhibitor: A Patent Review (2016-2020). Recent Pat Anticancer Drug Discov. 2021 Jul 28; doi: 10.2174/1574892816666210728125224. Epub 2021 Jul 28. PMID: 34323202.
Copy Download .nbib Format: NLM
Share it on

Recent Pat Anticancer Drug Discov. 2021 Jul 28; doi: 10.2174/1574892816666210728125224. Epub 2021 Jul 28.

An Update of Lysine Specific Demethylase 1 Inhibitor: A Patent Review (2016-2020).

Recent patents on anti-cancer drug discovery

Yi-Chao Zheng, Yue-Jiao Liu, Ya Gao, Bo Wang, Hong-Min Liu

Affiliations

  1. 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 Province 450001, China.

PMID: 34323202 DOI: 10.2174/1574892816666210728125224

Abstract

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 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 in vitro and in vivo. These patents exhibited the structural diversity of LSD1 inhibitors and the potential of natural products as novel LSD1 inhibitors.

Copyright© Bentham Science Publishers; For any queries, please email at [email protected].

Keywords: LSD1; cancer; derivatives; patent analysis; selective inhibitors; tranylcypromine

Publication Types