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Application of MassSQUIRM for Quantitative Measurements of Lysine Demethylase Activity
Published on: March 11, 2012
An Update of Lysine Specific Demethylase 1 Inhibitor: A Patent Review (2016-2020)
Yi-Chao Zheng1,2, Yue-Jiao Liu1,2, Ya Gao1,2
1Key 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.
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 in vitro and in vivo. These patents exhibited the structural diversity of LSD1 inhibitors and the potential of natural products as novel LSD1 inhibitors.
Insights
Recent patents reveal diverse lysine-specific demethylase 1 (LSD1) inhibitors, including Tranylcypromine derivatives and natural products, showing promising anticancer activity. These findings offer valuable insights for developing novel LSD1 modulators with improved efficacy and safety.
Area of Science:
- Oncology
- Medicinal Chemistry
- Drug Discovery
Background:
- Lysine-specific demethylase 1 (LSD1), a FAD-dependent enzyme, is overexpressed in various cancers.
- LSD1 regulates gene transcription linked to cancer development, making it a therapeutic target.
- Targeting LSD1 with inhibitors presents a novel strategy for anticancer drug development.
Purpose of the Study:
- To review patents on LSD1 inhibitors published within the last five years.
- To provide a reference for researchers developing potent and safe LSD1 modulators.
- To highlight structural diversity and therapeutic potential of emerging LSD1 inhibitors.
Main Methods:
- Systematic patent search using Espacenet®, Google Patents, and CNKI databases.
- Inclusion of patents disclosing LSD1 inhibitors since 2016.
- Analysis of compound structures and reported biological activities.
Main Results:
- Dozens of patents related to LSD1 inhibitors were identified from the past five years.
- Compound structures encompass Tranylcypromine derivatives, imidazole, pyrimidine derivatives, natural products, and peptides.
- Several compounds have advanced to clinical trials, demonstrating therapeutic progression.
Conclusions:
- Compounds in reviewed patents exhibit significant in vitro and in vivo antitumor activity.
- The structural diversity of LSD1 inhibitors is evident, with natural products showing promise.
- Patent landscape indicates active research and development in LSD1-targeted cancer therapies.
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