Abstract
Proteasome inhibition is a modern and surprisingly successful approach how to cancer treatment. Bortezomib (Velcade®) is a first-in-class proteasome inhibitor and has been approved for first-line treatment of multiple myeloma and second-line treatment of mantle cell lymphoma. There have been almost 200 clinical trials with bortezomib, both as a single agent and in combination with other drugs, for various cancers, as listed in the US National Cancer Institute database. However, bortezomibs mechanism of action remains elusive despite enormous progress in our knowledge of the cell biology of the ubiquitin-proteasome system (UPS) and bortezomibinduced signaling events in cancer cells. This review maps a rapidly growing and open body of research in both areas.
Keywords: Ubiquitin-proteasome system, bortezomib, mechanism of action, ubiquitin-proteasome, myeloma, lymphoma, aldehyde, calpain, murine, myelogenous, leukemia, tumorigenesis, tyrosine, deacetylases, polymerase, angiogenesis, emesis
Current Pharmaceutical Design
Title: The Ubiquitin-Proteasome System (UPS) and the Mechanism of Action of Bortezomib
Volume: 17 Issue: 15
Author(s): Boris Cvek and Zdenek Dvorak
Affiliation:
Keywords: Ubiquitin-proteasome system, bortezomib, mechanism of action, ubiquitin-proteasome, myeloma, lymphoma, aldehyde, calpain, murine, myelogenous, leukemia, tumorigenesis, tyrosine, deacetylases, polymerase, angiogenesis, emesis
Abstract: Proteasome inhibition is a modern and surprisingly successful approach how to cancer treatment. Bortezomib (Velcade®) is a first-in-class proteasome inhibitor and has been approved for first-line treatment of multiple myeloma and second-line treatment of mantle cell lymphoma. There have been almost 200 clinical trials with bortezomib, both as a single agent and in combination with other drugs, for various cancers, as listed in the US National Cancer Institute database. However, bortezomibs mechanism of action remains elusive despite enormous progress in our knowledge of the cell biology of the ubiquitin-proteasome system (UPS) and bortezomibinduced signaling events in cancer cells. This review maps a rapidly growing and open body of research in both areas.
Export Options
About this article
Cite this article as:
Cvek Boris and Dvorak Zdenek, The Ubiquitin-Proteasome System (UPS) and the Mechanism of Action of Bortezomib, Current Pharmaceutical Design 2011; 17 (15) . https://dx.doi.org/10.2174/138161211796197124
DOI https://dx.doi.org/10.2174/138161211796197124 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
- 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
-
Kit: Molecule of Interest for the Diagnosis and Treatment of Mastocytosis and other Neoplastic Disorders
Current Cancer Drug Targets Application of Phage Display Technology to Cancer Research
Current Pharmaceutical Biotechnology Immunotherapy-Based Strategies for the Treatment of Autoimmune Diabetes: Searching for the Cure
Current Pharmaceutical Design Genetic Variations in Telomere Maintenance, with Implications on Tissue Renewal Capacity and Chronic Disease Pathologies
Current Pharmacogenomics and Personalized Medicine Editorial(Hot Topic:Targeting the Ubiquitin-Proteasome Pathway - Current Perspectives and Future Directions)
Current Pharmaceutical Design Immune Modulation by Ionizing Radiation and its Implications for Cancer Immunotherapy
Current Pharmaceutical Design Potassium Channels: Novel Emerging Biomarkers and Targets for Therapy in Cancer
Recent Patents on Anti-Cancer Drug Discovery Repair and Translesion DNA Polymerases as Anticancer Drug Targets
Anti-Cancer Agents in Medicinal Chemistry Current Options in the Treatment of Mast Cell Mediator-Related Symptoms in Mastocytosis
Inflammation & Allergy - Drug Targets (Discontinued) Voltage-Gated Sodium Channels: New Targets in Cancer Therapy?
Current Pharmaceutical Design Synthesis and Biological Evaluation of a Novel Apogossypolone Derivative
Letters in Drug Design & Discovery Cancer Therapy By Targeting Hypoxia-Inducible Factor-1
Current Cancer Drug Targets Selenium Compounds Biotransformed by Mushrooms: Not Only Dietary Sources, But Also Toxicity Mediators
Current Nutrition & Food Science Innovative Targets For Asthma And COPD: Exploring The Existing And Screening The New!!
Infectious Disorders - Drug Targets Pharmacological Activity of Natural Non-glycosylated Triterpenes
Mini-Reviews in Organic Chemistry JAK2 Inhibitors for Myelofibrosis: Why are They Effective in Patients with and Without JAK2V617F Mutation?
Anti-Cancer Agents in Medicinal Chemistry Marine Natural Products and Related Compounds as Anticancer Agents: an Overview of their Clinical Status
Anti-Cancer Agents in Medicinal Chemistry Targeting the Immune Niche within the Bone Marrow Microenvironment: The Rise of Immunotherapy in Multiple Myeloma
Current Cancer Drug Targets Protein Modification by β-N-Acetyl Glucosamine (O-GlcNAc) in Insulin Signaling and Insulin Resistance
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery (Discontinued) Deciphering the Physiology Underlying the Rapid Clinical Effects of Perispinal Etanercept in Alzheimers Disease
Current Alzheimer Research