Abstract
Background: In the past few years, great of attention has been paid to the identification and characterization of selective and potent inhibitors of the first identified histone demethylase LSD1, which may erase mono- and di-methylated histone 3 lysine 4 and 9. As the aberrant overexpression of LSD1 is involved in various pathological processes, especially cancer, obtaining selective and potent LSD1 inhibitors has emerged as a crucial issue in medicinal chemistry research.
Method: Until now, several LSD1 inhibitor screening models have been established, including enzyme coupled assay, LC-MS based assay, and FRET based assay. Nevertheless, due to some special instrument requirement and additional costs of LC-MS and FRET, the enzyme coupled assay is the most widely applied method for LSD1 inhibitor screening. Result: We summarized and compared several reported in vitro LSD1 inhibitor screening models. Each of them has distinct advantages and disadvantages, and none of these methods is perfect. In order to exclude the false positive results, at least one additional method should be applied to screen LSD1 inhibitors.Keywords: LSD1, inhibitor, screening model, enzyme coupled assay, LC-MS, FRET.
Current Medicinal Chemistry
Title:An Overview on Screening Methods for Lysine Specific Demethylase 1 (LSD1) Inhibitors
Volume: 24 Issue: 23
Author(s): Yi-Chao Zheng, Jiao Chang, Ting Zhang , Feng-Zhi Suo , Xiao-Bing Chen, Ying Liu , Bing Zhao, Bin Yu*Hong-Min Liu*
Affiliation:
- School of Pharmaceutical Sciences, Zhengzhou University, P.O. Box: 450001, Zhengzhou,China
- School of Pharmaceutical Sciences, Zhengzhou University, P.O. Box: 450001, Zhengzhou,China
Keywords: LSD1, inhibitor, screening model, enzyme coupled assay, LC-MS, FRET.
Abstract: Background: In the past few years, great of attention has been paid to the identification and characterization of selective and potent inhibitors of the first identified histone demethylase LSD1, which may erase mono- and di-methylated histone 3 lysine 4 and 9. As the aberrant overexpression of LSD1 is involved in various pathological processes, especially cancer, obtaining selective and potent LSD1 inhibitors has emerged as a crucial issue in medicinal chemistry research.
Method: Until now, several LSD1 inhibitor screening models have been established, including enzyme coupled assay, LC-MS based assay, and FRET based assay. Nevertheless, due to some special instrument requirement and additional costs of LC-MS and FRET, the enzyme coupled assay is the most widely applied method for LSD1 inhibitor screening. Result: We summarized and compared several reported in vitro LSD1 inhibitor screening models. Each of them has distinct advantages and disadvantages, and none of these methods is perfect. In order to exclude the false positive results, at least one additional method should be applied to screen LSD1 inhibitors.Export Options
About this article
Cite this article as:
Zheng Yi-Chao , Chang Jiao , Zhang Ting, Suo Feng-Zhi , Chen Xiao-Bing , Liu Ying , Zhao Bing , Yu Bin *, Liu Hong-Min*, An Overview on Screening Methods for Lysine Specific Demethylase 1 (LSD1) Inhibitors, Current Medicinal Chemistry 2017; 24 (23) . https://dx.doi.org/10.2174/0929867324666170509114321
DOI https://dx.doi.org/10.2174/0929867324666170509114321 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Targeting Histone Deacetylase Inhibitors for Anti-Malarial Therapy
Current Topics in Medicinal Chemistry Mechanism of Action and Therapeutic Potential of Novel Adamantyl Retinoid-Related Molecules
Current Cancer Therapy Reviews Modulation of the Immune Response by Targeting Endothelial Cells
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Editorial from Guest Editor (Thematic Issue: Current Approach to COPD Management: Setting a Model in Medical Therapeutics)
Current Respiratory Medicine Reviews Perspectives in Nanomedicine-Based Research Towards Cancer Therapies
Current Nanoscience Potential Interactions of Carotenoids with Other Bioactive Food Components in the Prevention of Chronic Diseases
Current Bioactive Compounds Pathway Analysis for Design of Promiscuous Drugs and Selective Drug Mixtures
Current Drug Discovery Technologies Safety of Multi-Targeted Kinase Inhibitors as Monotherapy Treatment of Cancer: A Systematic Review of the Literature
Current Drug Safety Virtual Combinatorial Library Design, Synthesis and In vitro Anticancer Assessment of -2-Amino-3-Cyanopyridine Derivatives
Combinatorial Chemistry & High Throughput Screening Viability of Nanostructured Lipid Carrier System in Overcoming the Barriers Associated with Chemotherapeutic Delivery
Current Nanoscience The Emerging Role of EMT-related lncRNAs in Therapy Resistance and their Applications as Biomarkers
Current Medicinal Chemistry Immunotherapy for Myeloproliferative Neoplasms (MPN)
Current Cancer Drug Targets LHRH-Targeted Drug Delivery Systems for Cancer Therapy
Mini-Reviews in Medicinal Chemistry Evolution and Pathogenesis of Oncoviruses Associated with Head and Neck Cancer: History and Current Concepts
Recent Patents on Biomarkers The Klf6 Super-enhancer Determines Klf6 Sensitivity to BRD4 Inhibitors in Human Hepatoma (HepG2) Cells
Current Biotechnology Development of Vascular Endothelial Growth Factor Receptor (VEGFR) Kinase Inhibitors as Anti-Angiogenic Agents in Cancer Therapy
Current Medicinal Chemistry Interfering with Protein-Protein Contact: Molecular Interaction Maps and Peptide Modulators
Current Topics in Medicinal Chemistry The Significance of Ubiquitin Proteasome Pathway in Cancer Development
Recent Patents on Anti-Cancer Drug Discovery Progress in the Understanding of the Immune Microenvironment and Immunotherapy in Malignant Pleural Mesothelioma
Current Drug Targets A Novel Approach to the Technique of Lung Region Segmentation Based on a Deep Learning Model to Diagnose COVID-19 X-ray Images
Current Medical Imaging