Abstract
Deubiquitinating enzymes (or DUBs) attack the ubiquitin-based isopeptide bond, thus counteracting ubiquitinprotein ligase activity in vivo. By disassembling ubiquitin-substrate and ubiquitin-ubiquitin covalent links, deubiquitinating enzymes exert a very powerful control of many signaling processes within the ubiquitin-proteasome system (UPS). Very active research in this field in the last decade shows that deubiquitinating enzymes play important regulatory roles in aspects relevant to cancer, such as proteasome activity, p53 stability, the regulation of fanconi anemia related proteins, tumor cell apoptosis induction, to mention a few. Thus, deubiquitinating enzymes have emerged as interesting drug targets in cancer research. Here, the pharmacological inhibition of DUBs and its potential effect in cancer treatment are reviewed.
Keywords: Deubiquitinating enzymes, DUBs, inhibitors, proteasome, small-molecule, ubiquitin specific proteases, USP1, USP7, USP8, USP9x, USP14.
Current Cancer Drug Targets
Title:Deubiquitinating Enzyme Inhibitors and their Potential in Cancer Therapy
Volume: 14 Issue: 6
Author(s): Bernat Crosas
Affiliation:
Keywords: Deubiquitinating enzymes, DUBs, inhibitors, proteasome, small-molecule, ubiquitin specific proteases, USP1, USP7, USP8, USP9x, USP14.
Abstract: Deubiquitinating enzymes (or DUBs) attack the ubiquitin-based isopeptide bond, thus counteracting ubiquitinprotein ligase activity in vivo. By disassembling ubiquitin-substrate and ubiquitin-ubiquitin covalent links, deubiquitinating enzymes exert a very powerful control of many signaling processes within the ubiquitin-proteasome system (UPS). Very active research in this field in the last decade shows that deubiquitinating enzymes play important regulatory roles in aspects relevant to cancer, such as proteasome activity, p53 stability, the regulation of fanconi anemia related proteins, tumor cell apoptosis induction, to mention a few. Thus, deubiquitinating enzymes have emerged as interesting drug targets in cancer research. Here, the pharmacological inhibition of DUBs and its potential effect in cancer treatment are reviewed.
Export Options
About this article
Cite this article as:
Crosas Bernat, Deubiquitinating Enzyme Inhibitors and their Potential in Cancer Therapy, Current Cancer Drug Targets 2014; 14 (6) . https://dx.doi.org/10.2174/1568009614666140725090620
DOI https://dx.doi.org/10.2174/1568009614666140725090620 |
Print ISSN 1568-0096 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
Call for Papers in Thematic Issues
Advances in Cancer Biomarkers and Potential Drug Targets: From Diagnosis to Therapy
Cancer biomarkers play a crucial role in the diagnosis, prognosis, and treatment of cancer. They provide valuable information for cancer detection, risk assessment, treatment selection, and monitoring response to therapy. With advancements in molecular biology and high-throughput technologies, there has been an increasing interest in identifying and characterizing cancer biomarkers ...read more
Novel Therapeutic Approaches to Target Drug Resistant Tumors
With the development of disciplines such as chemical biology and molecular biology, the genes or proteins closely related to tumor occurrence and development have gradually become clear. Targeted therapies targeting these genes or proteins provide more effective methods for tumor treatment. Tumor targeted drugs generally only act on specific targets ...read more
ROLE OF IMMUNE AND GENOTOXIC RESPONSE BIOMARKERS IN TUMOR MICROENVIRONMENT IN CANCER DIAGNOSIS AND TREATMENT
Biological biomarkers have been used in medical research as an indicator of a normal or abnormal process inside the body, or of a disease. Nowadays, various researchers are in process to explore and investigate the biological markers for the early assessment of cancer. DNA Damage response (DDR) pathways and immune ...read more
Targeting the battlefield between host and tumor: basic research and clinical practice on reshaping tumor immune microenvironment
Immune system protects host against malignant tumors through effector cells and molecules. Cancer development and its response to therapy are regulated by inflammation, which either promotes or suppresses cancer progression. Chronic inflammation facilitates cancer progression and treatment resistance, whereas induction of acute inflammatory reactions often lead to anti-cancer immune responses. ...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
-
Review: Recent Clinical Trials in Epigenetic Therapy
Reviews on Recent Clinical Trials Non Peptidic Ligands at the Opioid Receptor Like-1 (ORL-1)
Mini-Reviews in Medicinal Chemistry Protein Kinase B/AKT and Focal Adhesion Kinase: Two Close Signaling Partners in Cancer
Anti-Cancer Agents in Medicinal Chemistry How Would Composite Traditional Chinese Medicine Protect the Brain – An Example of the Composite Formula “Pien Tze Huang”
Current Medicinal Chemistry Multiple Protective Functions of Sigma1 Receptor
Current Protein & Peptide Science Is C-Peptide Replacement the Missing Link for Successful Treatment of Neurological Complications in Type 1 Diabetes?
Current Drug Targets EGFR Transactivation by Peptide G Protein-Coupled Receptors in Cancer
Current Drug Targets Neurotoxicity of β-Amyloid Protein: Oligomerization, Channel Formation and Calcium Dyshomeostasis
Current Pharmaceutical Design Cancer Stem Cells: How can we Target them?
Current Medicinal Chemistry Carbon-11 Labeled Tracers for In Vivo Imaging of P-Glycoprotein Function: Kinetics, Advantages and Disadvantages
Current Topics in Medicinal Chemistry A Prooxidant Mechanism for the Anticancer and Chemopreventive Properties of Plant Polyphenols
Current Drug Targets Pituitary Adenylate Cyclase Activating Polypeptide: A Potential Neuroprotective Peptide
Current Pharmaceutical Design Brain-Derived Neurotrophic Factor (BDNF) has Proliferative Effects on Neural Stem Cells through the Truncated TRK-B Receptor, MAP Kinase, AKT, and STAT-3 Signaling Pathways
Current Neurovascular Research Melatonin-mitochondria Interplay in Health and Disease
Current Topics in Medicinal Chemistry Anticancer Drugs in Liposomal Nanodevices: A Target Delivery for a Targeted Therapy
Current Topics in Medicinal Chemistry Recent Advances in Health Promoting Effect of Dietary Polyphenols
Current Nutrition & Food Science Development of Prodrugs for Enzyme-Mediated, Tumor-Selective Therapy
Current Medicinal Chemistry - Anti-Cancer Agents Nitric Oxide and Dopamine Neurons. Implications for Parkinsons Disease
Current Medicinal Chemistry - Central Nervous System Agents Brain Nitric Oxide and Its Dual Role in Neurodegeneration / Neuroprotection: Understanding Molecular Mechanisms to Devise Drug Approaches
Current Medicinal Chemistry Neuroprotection & Mechanism of Ethanol in Stroke and Traumatic Brain Injury Therapy: New Prospects for an Ancient Drug
Current Drug Targets