Abstract
Background: Regardless of contemporary improvements in cancer treatment, the results of drugtreatment are not always efficacious. Thus, the development of novel approaches that affect cancer cell-specificmetabolic pathways is needed. Since much evidence has shown that tumor cell proliferation and motility arestimulated by glutamate via activation of its receptors, use of antagonists to these receptors may be the key tocontrol cancer cell progression. Riluzole noncompetitive metabotropic glutamate receptor 1 (mGluR1) antagonist,commonly used to treat patients with amyotrophic lateral sclerosis (ALS), has shown some antineoplasticproperties against melanoma, breast and prostate cancer. Yet little is known about its molecular mode of action.
Aims: The current study aims at evaluating the abilities of Riluzole to inhibit proliferation of several cancer celllines, as well as resolve the mechanism of its action.
Method: We demonstrated antiproliferative and antimigrative properties of Riluzole in rhabdomyosarcomamedulloblastoma,neuroblastoma, astrocytoma, glioma, colon cancer, lung cancer, thyroid carcinoma, leukemia,erythroleukemia and multiple myeloma. Our studies revealed apoptosis induction and G2-M cell cycle arrest inRiluzole treated A549, C6 and HT-29 cells.
Result: At the molecular level, we found that these cells treated with Riluzole had a decrease of Cyclin B and anincrease of p21 Waf1/Cip1 and p53 expression. We also observed an enhancement of CDK1 and Chk2 phosphorylation.Reported changes may suggest the involvement of these proteins in G2-M arrest, observed in flowcytometry analysis. These data indicated the potential use of Riluzole in the treatment of different types of cancers.
Keywords:Riluzole, proliferation, apoptosis, G2-M cell cycle arrest, migration, tumor.
Graphical Abstract
Anti-Cancer Agents in Medicinal Chemistry
Title:Riluzole Inhibits Proliferation, Migration and Cell Cycle Progression and Induces Apoptosis in Tumor Cells of Various Origins
Volume: 18Issue: 4
Author(s):Marta Kinga Lemieszek*, Andrzej Stepulak, Katarzyna Sawa-Wejksza, Arkadiusz Czerwonka, Chrysanthy Ikonomidou and Wojciech Rzeski
Affiliation:
- Department of Medical Biology, Institute of Agricultural Medicine, 20-090 Lublin,Poland
Keywords:Riluzole, proliferation, apoptosis, G2-M cell cycle arrest, migration, tumor.
Abstract: Background: Regardless of contemporary improvements in cancer treatment, the results of drugtreatment are not always efficacious. Thus, the development of novel approaches that affect cancer cell-specificmetabolic pathways is needed. Since much evidence has shown that tumor cell proliferation and motility arestimulated by glutamate via activation of its receptors, use of antagonists to these receptors may be the key tocontrol cancer cell progression. Riluzole noncompetitive metabotropic glutamate receptor 1 (mGluR1) antagonist,commonly used to treat patients with amyotrophic lateral sclerosis (ALS), has shown some antineoplasticproperties against melanoma, breast and prostate cancer. Yet little is known about its molecular mode of action.
Aims: The current study aims at evaluating the abilities of Riluzole to inhibit proliferation of several cancer celllines, as well as resolve the mechanism of its action.
Method: We demonstrated antiproliferative and antimigrative properties of Riluzole in rhabdomyosarcomamedulloblastoma,neuroblastoma, astrocytoma, glioma, colon cancer, lung cancer, thyroid carcinoma, leukemia,erythroleukemia and multiple myeloma. Our studies revealed apoptosis induction and G2-M cell cycle arrest inRiluzole treated A549, C6 and HT-29 cells.
Result: At the molecular level, we found that these cells treated with Riluzole had a decrease of Cyclin B and anincrease of p21 Waf1/Cip1 and p53 expression. We also observed an enhancement of CDK1 and Chk2 phosphorylation.Reported changes may suggest the involvement of these proteins in G2-M arrest, observed in flowcytometry analysis. These data indicated the potential use of Riluzole in the treatment of different types of cancers.
Export Options
About this article
Cite this article as:
Lemieszek Kinga Marta *, Stepulak Andrzej , Sawa-Wejksza Katarzyna , Czerwonka Arkadiusz , Ikonomidou Chrysanthy and Rzeski Wojciech , Riluzole Inhibits Proliferation, Migration and Cell Cycle Progression and Induces Apoptosis in Tumor Cells of Various Origins, Anti-Cancer Agents in Medicinal Chemistry 2018; 18 (4) .https://dx.doi.org/10.2174/1871520618666180228152713
| DOI https://dx.doi.org/10.2174/1871520618666180228152713 | Print ISSN 1871-5206 |
| Publisher Name Bentham Science Publisher | Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Advances in Nanomedicines and Targeted Therapies for Colorectal Cancer
Colorectal cancer remains a significant global health challenge, with high incidence and mortality rates despite advancements in treatment strategies. Conventional therapies often face limitations such as systemic toxicity, drug resistance, and suboptimal targeting. The advent of nanomedicines and innovative drug delivery systems offers new hope for overcoming these challenges and ...read more
Designing Novel Molecules for Anti-Cancer Enzyme Modulation: A Mechanistic and Therapeutic Perspective
The deficiencies or hyper functions of enzymes cause a number of diseases. Enzyme inhibition is an important area of pharmaceutical research since studies in this field have already led to the discovery of wide variety of drugs useful in a number of diseases. Specific inhibitors interact with enzymes and block ...read more
Discovery of Lead compounds targeting transcriptional regulation
Transcriptional regulation plays key physiological functions in body growth and development. Transcriptional dysregulation is one of the 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 ...read more
Heterocyclic Systems: Bridging Chemistry and Biology in Cancer Therapy
The thematic issue, "Heterocyclic Systems: Bridging Chemistry and Biology in Cancer Therapy," explores the critical role of heterocyclic compounds in advancing the frontiers of cancer treatment. Heterocycles serve as fundamental building blocks in medicinal chemistry due to their structural diversity and ability to interact with biological targets. This issue aims ...read more
Related Journals
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry
Current Analytical Chemistry
Current Computer-Aided Drug Design
Current Bioactive Compounds
Current Cancer Drug Targets
Combinatorial Chemistry & High Throughput Screening
Current Cancer Therapy Reviews
Current Diabetes Reviews
Current Drug Safety
Current Drug Targets
Related Books
Therapeutic Plants: Recent Advances in the Use of Herbs as Alternative Medications
Quality Assurance of Ethno-Herbals: Cultivating Confidence in Alternative Medicine
Ionic Liquids for Organic Synthesis
Traditional Medicine in North East Africa: Research on Traditional Healer Preparations and Herbs
Nanomaterials in Glioblastoma Research, Diagnosis and Therapy
Glycals and their Derivatives
Advancements in Cancer Research: Exploring Diagnostics and Therapeutic Breakthroughs
Organic Spectroscopy Technology and Applications
Andrographolide and its Analogs: Botanical Sources, Phytochemistry, Pharmacology, and Biotechnology
Metabolites of Medicinal Plants: Insightful Approaches
73
8
1
- Author Guidelines
- Bentham Author Support Services (BASS)
- 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
- A Novel Lily-of-the-Valley Fragrance Contrast Agent for Magnetic Resonance and Fluorescence Imaging of Prostate Cancer Cells
Current Pharmaceutical Biotechnology Mechanism of Action of Volatile Anesthetics: Involvement of Intracellular Calcium Signaling
Current Drug Targets - CNS & Neurological Disorders Epigenetics: Relations to Disease and Laboratory Findings
Current Medicinal Chemistry Cancer Stem Cells and the Biology of Brain Tumors
Current Stem Cell Research & TherapyNanomedicine Based Nanoparticles for Neurological Disorders
Current Medicinal ChemistryThe Potential Role of Peritumoral Apparent Diffusion Coefficient Evaluation in Differentiating Glioblastoma and Solitary Metastatic Lesions of the Brain
Current Medical ImagingThe Role of 3D Pharmacophore Mapping Based Virtual Screening for Identification of Novel Anticancer Agents: An Overview
Current Topics in Medicinal ChemistryHow do Glial Cells Contribute to Motor Control?
Current Pharmaceutical Design Rational Drug Development Using Gene-Targeted Agents and Their Application in Anti-Gene Radiotherapy
Current GenomicsAnti-Gene IGF-I Vaccines in Cancer Gene Therapy: A Review of aCase of Glioblastoma
Current Medicinal ChemistryHarnessing Phage Display for the Discovery of Peptide-Based Drugs and Monoclonal Antibodies
Current Medicinal Chemistry Regulatory T Cells: Major Players in the Tumor Microenvironment
Current Pharmaceutical DesignPotential Impacts of Prebiotics and Probiotics on Cancer Prevention
Anti-Cancer Agents in Medicinal ChemistryPeptide Therapeutics in Neurodegenerative Disorders
Current Medicinal ChemistryMMPs in Ovarian Cancer as Therapeutic Targets
Anti-Cancer Agents in Medicinal ChemistryMultiple Means by Which Nitric Oxide can Antagonize Photodynamic Therapy
Current Medicinal ChemistryCurcumin and its Derivatives: Their Application in Neuropharmacology and Neuroscience in the 21st Century
Current NeuropharmacologyTrends in Malignant Glioma Monoclonal Antibody Therapy
Current Cancer Therapy ReviewsCombined Anticancer Therapies: An Overview of the Latest Applications
Anti-Cancer Agents in Medicinal Chemistry 1-Cyclohexylpiperazine and 3,3-Dimethylpiperidine Derivatives as Sigma-1 (σ1) and Sigma-2 (σ2) Receptor Ligands: A Review
Central Nervous System Agents in Medicinal Chemistry
[8]ページ先頭