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 |
- 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
-
Medicinal and Beneficial Health Applications of Tinospora cordifolia (Guduchi): A Miraculous Herb Countering Various Diseases/Disorders and its Immunomodulatory Effects
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Immunological Approaches to Prevent Neuronal Apoptosis During Neuroinflammation
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents Proton Magnetic Resonance Spectroscopy Changes After Antipsychotic Treatment
Current Medicinal Chemistry Prospects for Plant-Derived Chemopreventive Agents Exhibiting Multiple Mechanisms of Action
Current Medicinal Chemistry - Anti-Cancer Agents Cyclin-Dependent Kinase 4/6 (Cdk4/6) Inhibitors: Perspectives in Cancer Therapy and Imaging
Mini-Reviews in Medicinal Chemistry Promising Targets in Anti-cancer Drug Development: Recent Updates
Current Medicinal Chemistry Heat Shock Proteins: Therapeutic Drug Targets for Chronic Neurodegeneration?
Current Pharmaceutical Biotechnology Intrahypothalamic Administration of Modafinil Increases Expression of MAP-Kinase in Hypothalamus and Pons in Rats
CNS & Neurological Disorders - Drug Targets Screening Neuroprotective Agents Through 4-hydroxynonenal, Ethanol, High Glucose, Homocysteine, Okadaic Acid, Rotenone, and Oxygen-Glucose Deprivation Induced PC12 Injury Models: A Review
Current Psychopharmacology General Anesthetics in Pediatric Anesthesia: Influences on the Developing Brain
Current Drug Targets Benzofuran Small Molecules as Potential Inhibitors of Human Protein Kinases. A Review
Current Pharmaceutical Design Papillary Thyroid Carcinoma in Pediatric Age: An Example of a Rare Tumour Managed Within a Cooperative Comprehensive Project
Current Pediatric Reviews Integrins in Drug Targeting-RGD Templates in Toxins
Current Pharmaceutical Design Targeting Tumor Ubiquitin-Proteasome Pathway with Polyphenols for Chemosensitization
Anti-Cancer Agents in Medicinal Chemistry The Cytoskeleton as a Therapeutic Target in Childhood Acute Leukemia:Obstacles and Opportunities
Current Drug Targets Targeting the p53-Family in Cancer and Chemosensitivity: Triple Threat
Current Drug Targets Small Molecular Inhibitors Targeting Chromatin Regulating Proteins for Cancer
Current Protein & Peptide Science Resisting the Resistance in Cancer: Cheminformatics Studies on Short- Path Base Excision Repair Pathway Antagonists Using Supervised Learning Approaches
Combinatorial Chemistry & High Throughput Screening Cerebrospinal Fluid Proteomes: From Neural Development to Neurodegenerative Diseases
Current Proteomics Multi-Nuclear Platinum Drugs: A New Paradigm in Chemotherapy
Current Medicinal Chemistry - Anti-Cancer Agents