Abstract
The Langmuir monolayer technique is one of the methods used to build models of cellular membranes and enables to investigate the interactions of membrane components with other biomolecules. This method has been applied to study the effect of edelfosine - a synthetic alkyl-lysophospholipid analog - on model lipid membranes in order to get insight into its mode of action and selectivity. Edelfosine is mainly known for its anticancer properties, although it is also applied in the treatment of other diseases, like autoimmune, anti-HIV and antiparasitic. In this review we focus on its antitumor activity (although some other aspects of its therapeutic effects are also indicated) and summarize the results obtained so far with use of the monolayer technique. The application of this method evidenced for a key role of cholesterol and membrane rafts in the mechanism of anticancer activity of edelfosine. As regards the selectivity of this drug, the obtained results proved that the difference in fluidity of tumor versus normal cell membrane is important but probably not the only factor determining an easier incorporation of edelfosine into cancer cells. Further studies show that edelfosine is of strong affinity to gangliosides, which may be considered as molecules targeting edelfosine into cancer cell membrane.
Keywords: Edelfosine, interactions, langmuir monolayers, model lipids membranes.
Anti-Cancer Agents in Medicinal Chemistry
Title:Edelfosine in Membrane Environment - the Langmuir Monolayer Studies
Volume: 14 Issue: 4
Author(s): Patrycja Dynarowicz-Latka and Katarzyna Hac-Wydro
Affiliation:
Keywords: Edelfosine, interactions, langmuir monolayers, model lipids membranes.
Abstract: The Langmuir monolayer technique is one of the methods used to build models of cellular membranes and enables to investigate the interactions of membrane components with other biomolecules. This method has been applied to study the effect of edelfosine - a synthetic alkyl-lysophospholipid analog - on model lipid membranes in order to get insight into its mode of action and selectivity. Edelfosine is mainly known for its anticancer properties, although it is also applied in the treatment of other diseases, like autoimmune, anti-HIV and antiparasitic. In this review we focus on its antitumor activity (although some other aspects of its therapeutic effects are also indicated) and summarize the results obtained so far with use of the monolayer technique. The application of this method evidenced for a key role of cholesterol and membrane rafts in the mechanism of anticancer activity of edelfosine. As regards the selectivity of this drug, the obtained results proved that the difference in fluidity of tumor versus normal cell membrane is important but probably not the only factor determining an easier incorporation of edelfosine into cancer cells. Further studies show that edelfosine is of strong affinity to gangliosides, which may be considered as molecules targeting edelfosine into cancer cell membrane.
Export Options
About this article
Cite this article as:
Dynarowicz-Latka Patrycja and Hac-Wydro Katarzyna, Edelfosine in Membrane Environment - the Langmuir Monolayer Studies, Anti-Cancer Agents in Medicinal Chemistry 2014; 14 (4) . https://dx.doi.org/10.2174/1871520614666140309230722
DOI https://dx.doi.org/10.2174/1871520614666140309230722 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Discovery of Lead compounds targeting transcriptional regulation
Transcriptional regulation plays key physiological functions in body growth and development. Transcriptional dysregulation is one of important biomarkers of tumor genesis and progression, which is involved in regulating tumor cell processes such as cell proliferation, differentiation, and apoptosis. Additionally, it plays a pivotal role in angiogenesis and promotes tumor metastasis ...read more
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Innovative targets in medicinal chemistry
Medicinal chemistry continuously evolves in response to emerging healthcare needs and advancements in scientific understanding. This special issue explores the current landscape of innovative targets in medicinal chemistry, highlighting the quest for novel therapeutic avenues. From traditional drug targets such as enzymes and receptors to emerging targets like protein-protein interactions ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...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
Related Articles
-
Studies on Chloride Channels and their Modulators
Current Topics in Medicinal Chemistry Natural Products as a Source of Protein Kinase Activators and Inhibitors
Current Topics in Medicinal Chemistry Electrocatalytic Determination of 6-Mercaptopurine Using Multiwall Carbon Nanotubes Paste Electrode in the Presence of Methyldopa
Current Nanoscience E2F1 and NF-κB: Key Mediators of Inflammation-associated Cancers and Potential Therapeutic Targets
Current Cancer Drug Targets Review on Documented Medicinal Plants used for the Treatment of Cancer
Current Traditional Medicine Synthesis and Evaluation of 2-Substituted Fendiline Analogues as Antileukemics
Letters in Drug Design & Discovery Threes Company: Regulation of Cell Fate by Statins
Current Drug Targets - Cardiovascular & Hematological Disorders Muscarinic Acetylcholine Receptor-Interacting Proteins (mAChRIPs): Targeting the Receptorsome
Current Drug Targets Bisacylimidoselenocarbamates Cause G2/M Arrest Associated with the Modulation of CDK1 and Chk2 in Human Breast Cancer MCF-7 Cells
Current Medicinal Chemistry Erythropoietic Porphyrias: Animal Models and Update in Gene-Based Therapies
Current Gene Therapy Microwave-assisted Cycloaddition Reactions in Carbo- and Heterocyclic Chemistry
Current Organic Chemistry Chromatin Structure and Epigenetics of Tumour Cells: A Review
Cardiovascular & Hematological Disorders-Drug Targets Pro-apoptotic Activity of BH3-only Proteins and BH3 Mimetics: from Theory to Potential Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry miRNAs in Cancer Prevention and Treatment and as Molecular Targets for Natural Product Anticancer Agents
Current Cancer Drug Targets Clinical Pharmacogenomics of Thiopurine S-methyltransferase
Current Clinical Pharmacology Chemoradiotherapy of Human Tumors: Novel Approaches from Nanomedicine
Current Pharmaceutical Design Reversing Aberrant Methylation Patterns in Cancer
Current Medicinal Chemistry Novel Derivatives of Benfluron and Dimefluron Synthesis and Anticancer activity
Letters in Drug Design & Discovery From Leflunomide to Teriflunomide: Drug Development and Immunosuppressive Oral Drugs in the Treatment of Multiple Sclerosis
Current Neuropharmacology Caffeic Acid Phenethyl Ester Effects: In Silico Study of its Osteoimmunological Mechanisms
Letters in Drug Design & Discovery