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
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
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...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
-
Novel Immunotherapeutic Strategies for Invasive Fungal Disease
Current Drug Targets - Cardiovascular & Hematological Disorders Chronic Myelogenous Leukemia
Current Cancer Therapy Reviews HLA-G Expression in Cancers: Potential Role in Diagnosis, Prognosis and Therapy
Endocrine, Metabolic & Immune Disorders - Drug Targets Kavalactone Pharmacophores for Major Cellular Drug Targets
Mini-Reviews in Medicinal Chemistry Interaction of Human Brain Acetylcholinesterase with Cyclophosphamide: A Molecular Modeling and Docking Study
CNS & Neurological Disorders - Drug Targets Advanced Assessment of the Endogenous Hormone Level as a Potential Biomarker of the Urogenital Tract Cancer
Combinatorial Chemistry & High Throughput Screening Multifaceted Mechanisms for Cell Survival and Drug Targeting in Chronic Myelogenous Leukemia
Current Cancer Drug Targets Valproic Acid As Anti-Cancer Drug
Current Pharmaceutical Design Parallel Gene Expression Profiling of Mantle Cell Lymphoma – How Do We Transform ´Omics Data into Clinical Practice
Current Genomics Vascular Endothelial Growth Factor (VEGF) as a Target of Bevacizumab in Cancer: From the Biology to the Clinic
Current Medicinal Chemistry CD20-based Immunotherapy of B-cell Derived Hematologic Malignancies
Current Cancer Drug Targets Transcriptomic Effects of Estrogen Starvation and Induction in the MCF7 Cells. The Meta-analysis of Microarray Results
Current Pharmaceutical Biotechnology Alteration of the Proline at Position 7 of the HIV-1 Spacer Peptide p1 Suppresses Viral Infectivity in a Strain Dependent Manner
Current HIV Research The Use of Temozolomide for the Treatment of Malignant Tumors: Clinical Evidence and Molecular Mechanisms of Action
Recent Patents on Anti-Cancer Drug Discovery Resistance in Cancer: A Target for Drug Discovery
Current Medicinal Chemistry - Anti-Cancer Agents Aberrant Expression of MicroRNAs in B-cell Lymphomas
MicroRNA Laccases in Pharmaceutical Chemistry: A Comprehensive Appraisal
Mini-Reviews in Organic Chemistry Redox Homeostasis, Bioactive Agents and Transduction Therapy
Current Signal Transduction Therapy The Expanding Role of APRIL in Cancer and Immunity
Current Molecular Medicine Development of Novel Protein Scaffolds as Alternatives to Whole Antibodies for Imaging and Therapy: Status on Discovery Research and Clinical Validation
Current Pharmaceutical Biotechnology