Abstract
Tumours exhibit higher basal levels of reactive oxygen species (ROS) and altered redox environment compared to normal cells. Excessive level of ROS can be toxic to these cells, thus they become more vulnerable to damage by further ROS insults induced by pharmacological agents. However, the upregulation of antioxidant capacity in adaptation to intrinsic oxidative stress in cancer cells can confer drug resistance. Therefore, abrogation of such drugresistant mechanisms by redox modulation could have significant therapeutic implications. Many redox-modulating agents have been developed. The redox-active system epitomised by ascorbate-driven quinone redox cycling, and the group of redox-silent vitamin E analogues represented by α-tocopheryl succinate have been shown to induce selective cancer cell death in different types of cancer. These compounds synergistically act by destabilising organelles like mitochondria, unleashing their apoptogenic potential, which results in efficient death of malignant cells and suppression of tumour growth. Consistent with this notion, clinical trials that aim to examine the therapeutic performance of novel redoxmodulating drugs in cancer patients are currently under way.
Keywords: Apoptosis, autophagy, redox-active agents, redox-silent agent, ROS-based cancer therapy, vitamin E analogues.
Current Medicinal Chemistry
Title:Redox-active and Redox-silent Compounds: Synergistic Therapeutics in Cancer
Volume: 22 Issue: 5
Author(s): M. Tomasetti, L. Santarelli, R. Alleva, Lan-Feng Dong and J. Neuzil
Affiliation:
Keywords: Apoptosis, autophagy, redox-active agents, redox-silent agent, ROS-based cancer therapy, vitamin E analogues.
Abstract: Tumours exhibit higher basal levels of reactive oxygen species (ROS) and altered redox environment compared to normal cells. Excessive level of ROS can be toxic to these cells, thus they become more vulnerable to damage by further ROS insults induced by pharmacological agents. However, the upregulation of antioxidant capacity in adaptation to intrinsic oxidative stress in cancer cells can confer drug resistance. Therefore, abrogation of such drugresistant mechanisms by redox modulation could have significant therapeutic implications. Many redox-modulating agents have been developed. The redox-active system epitomised by ascorbate-driven quinone redox cycling, and the group of redox-silent vitamin E analogues represented by α-tocopheryl succinate have been shown to induce selective cancer cell death in different types of cancer. These compounds synergistically act by destabilising organelles like mitochondria, unleashing their apoptogenic potential, which results in efficient death of malignant cells and suppression of tumour growth. Consistent with this notion, clinical trials that aim to examine the therapeutic performance of novel redoxmodulating drugs in cancer patients are currently under way.
Export Options
About this article
Cite this article as:
Tomasetti M., Santarelli L., Alleva R., Dong Lan-Feng and Neuzil J., Redox-active and Redox-silent Compounds: Synergistic Therapeutics in Cancer, Current Medicinal Chemistry 2015; 22 (5) . https://dx.doi.org/10.2174/0929867321666140915142219
DOI https://dx.doi.org/10.2174/0929867321666140915142219 |
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
-
Discovery of Small Molecule c-Met Inhibitors: Evolution and Profiles of Clinical Candidates
Anti-Cancer Agents in Medicinal Chemistry Cerenkov Luminescence Imaging at a Glance
Current Molecular Imaging (Discontinued) The Potential Role of Pharmacogenomic and Genomic in the Adjuvant Treatment of Early Stage Non Small Cell Lung Cancer
Current Genomics Development of Heparanase Inhibitors for Anti-Cancer Therapy
Current Medicinal Chemistry From TGF-β to Cancer Therapy
Current Drug Targets Recent Patents on Heat Shock Proteins Targeting Antibodies
Recent Patents on Anti-Cancer Drug Discovery Potentials of Polymeric Nanoparticle as Drug Carrier for Cancer Therapy: With a Special Reference to Pharmacokinetic Parameters
Current Drug Metabolism Identification of AHSA1 as a Potential Therapeutic Target for Breast Cancer: Bioinformatics Analysis and <i>in vitro</i> Studies
Current Cancer Drug Targets Monofunctional Platinum (PtII) Compounds – Shifting the Paradigm in Designing New Pt-based Anticancer Agents
Current Medicinal Chemistry Modified cAMP Derivatives: Powerful Tools in Heart Research
Current Medicinal Chemistry Colloidal Polymeric Nanoparticles and Brain Drug Delivery
Current Drug Delivery Diffusion-Weighted Imaging in Abdominal Oncology
Current Medical Imaging Naturally-occurring Dimers of Flavonoids as Anticarcinogens
Anti-Cancer Agents in Medicinal Chemistry Molecular Imaging with Small Animal PET/CT
Current Medical Imaging Destroying RNA as a Therapeutic Approach
Current Medicinal Chemistry Prolyl-Specific Peptidases and Their Inhibitors in Biological Processes
Current Chemical Biology Tyrosine Kinases as Molecular Targets to Inhibit Cancer Progression and Metastasis
Current Pharmaceutical Design Exosomal miR-214-5p Released from Glioblastoma Cells Modulates Inflammatory Response of Microglia after Lipopolysaccharide Stimulation through Targeting CXCR5
CNS & Neurological Disorders - Drug Targets Double-Edged Sword of Novel Anti-Cancer Treatment: Proteasome Inhibition in the Growth Plate Causes Impairment of Longitudinal Bone Growth
Current Pediatric Reviews Delivery Methods of Camptothecin and Its Hydrosoluble Analogue Irinotecan for Treatment of Colorectal Cancer
Current Drug Delivery