Abstract
3-bromopyruvate (3-BrPA), a pyruvate analog recently proposed as a possible anticancer drug, was investigated in relation to its capacity to inhibit energy production in fractions obtained from normal cells (rat hepatocytes) and in isolated rat thymocytes. Findings were that main targets of the drug were glyceraldehyde 3-phosphate dehydrogenase, and not hexokinase as suggested for hepatoma cells, and succinate -driven ATP synthesis. Consistently with the above findings, in the normal cells studied (thymocytes) the drug elicited an important fall in ATP levels. The significance of the present findings in concern with a possible therapeutic usefulness of the drug is discussed.
Keywords: 3-Bromopyruvate, Warburg effect, tumor therapy, glycolysis, hexokinase, glyceraldehyde-3-phosphate dehydrogenase, oxidative phosphorylation, succinate dehydrogenase
Medicinal Chemistry
Title: Targets of 3-Bromopyruvate, A New, Energy Depleting, Anticancer Agent
Volume: 5 Issue: 6
Author(s): P. Dell'Antone
Affiliation:
Keywords: 3-Bromopyruvate, Warburg effect, tumor therapy, glycolysis, hexokinase, glyceraldehyde-3-phosphate dehydrogenase, oxidative phosphorylation, succinate dehydrogenase
Abstract: 3-bromopyruvate (3-BrPA), a pyruvate analog recently proposed as a possible anticancer drug, was investigated in relation to its capacity to inhibit energy production in fractions obtained from normal cells (rat hepatocytes) and in isolated rat thymocytes. Findings were that main targets of the drug were glyceraldehyde 3-phosphate dehydrogenase, and not hexokinase as suggested for hepatoma cells, and succinate -driven ATP synthesis. Consistently with the above findings, in the normal cells studied (thymocytes) the drug elicited an important fall in ATP levels. The significance of the present findings in concern with a possible therapeutic usefulness of the drug is discussed.
Export Options
About this article
Cite this article as:
Dell'Antone P., Targets of 3-Bromopyruvate, A New, Energy Depleting, Anticancer Agent, Medicinal Chemistry 2009; 5 (6) . https://dx.doi.org/10.2174/157340609790170551
DOI https://dx.doi.org/10.2174/157340609790170551 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
Call for Papers in Thematic Issues
Carbohydrates in Computational and Medicinal Chemistry
Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
Recent Advances in the Medicinal Chemistry of Cancer
Scope of the Thematic Issue: Correlation between structure and function is one of the important aspects of the success of anti-cancer compounds associated with their structure-activity interactions, physiology, biochemical, molecular, and genetic processes. Overcoming these obstacles is key to obtaining further insights into developments in rational drug design, bioorganic chemistry, ...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
-
Pharmacological Overview and Future Perspectives of Cholinergic Therapy in Alzheimers Disease
Current Drug Therapy Alzheimers Disease and Oxidative Stress: The Old Problem Remains Unsolved
Current Medicinal Chemistry - Central Nervous System Agents The Changing Landscape of Voltage-Gated Calcium Channels in Neurovascular Disorders and in Neurodegenerative Diseases
Current Neuropharmacology MicroRNA Involvement in the Pathogenesis of Neuroblastoma: Potential for MicroRNA Mediated Therapeutics
Current Pharmaceutical Design Peptides to Target Tumor Vasculature and Lymphatics for Improved Anti-Angiogenesis Therapy
Current Cancer Drug Targets Interactions of Iron Oxide Nanoparticles with the Immune System: Challenges and Opportunities for their Use in Nano-oncology
Current Pharmaceutical Design Evolution of Resistance to Cancer Therapy
Current Pharmaceutical Design The Effect of PDE5 Inhibitors on the Male Reproductive Tract
Current Pharmaceutical Design Histone Deacetylase Inhibitors: From Chromatin Remodeling to Experimental Cancer Therapeutics
Current Medicinal Chemistry Radiation Therapy Plus Angiogenesis Inhibition with Bevacizumab: Rationale and Initial Experience
Reviews on Recent Clinical Trials Indolo[2,3-a]quinolizidines and Derivatives: Bioactivity and Asymmetric Synthesis
Current Pharmaceutical Design Factors Interacting with HIF-1α mRNA: Novel Therapeutic Targets
Current Pharmaceutical Design Immunotherapy of Cancer Based on DC-Tumor Fusion Vaccine
Current Immunology Reviews (Discontinued) Anti-Angiogenic Therapies for Children with Cancer
Current Cancer Drug Targets Multimodality Imaging of RNA Interference
Current Medicinal Chemistry Novel Approaches for Modulating dUTPase and Uracil-DNA Glycosylase: Potential Uses for Cancer and Viral Chemotherapy
Drug Design Reviews - Online (Discontinued) Tumor Stroma as a Target in Cancer
Current Cancer Drug Targets Utilization of Lipid-based Nanoparticles to Improve the Therapeutic Benefits of Bortezomib
Anti-Cancer Agents in Medicinal Chemistry Ferric Cycle Activity and Alzheimer Disease
Current Neurovascular Research Epigenetic Drugs for Multiple Sclerosis
Current Neuropharmacology