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
-
Anti-Inflammatory and Pro-Resolving Effects of N-3 PUFA in Cancers: Structures and Mechanisms
Current Topics in Medicinal Chemistry Apoptosis-Induction is A Novel Therapeutic Strategy for Gastrointestinal and Liver Cancers
Current Gene Therapy Gynecomastia in Infants, Children, and Adolescents
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery How is Gene Transfection Able to Improve Current Chemotherapy? The Role of Combined Therapy in Cancer Treatment
Current Medicinal Chemistry Small Players With Big Roles: MicroRNAs as Targets to Inhibit Breast Cancer Progression
Current Drug Targets Development and Clinical Application of Peptide-Based Radiopharmaceuticals
Current Pharmaceutical Design Mechanisms of Melatonin in Alleviating Alzheimer’s Disease
Current Neuropharmacology Identification of Disease States and Response to Therapy in Humans by Utilizing the Biomarker EGFR for Targeted Molecular Imaging
Current Protein & Peptide Science A Review on the Monoacylglycerol Lipase: At the Interface Between Fat and Endocannabinoid Signalling
Current Medicinal Chemistry Targets for Anti-metastatic Drug Development
Current Pharmaceutical Design Dexamethasone Reduces Cell Adhesion and Migration of T47D Breast Cancer Cell Line
Anti-Cancer Agents in Medicinal Chemistry The Therapeutic Potential of Gallium-Based Complexes in Anti-Tumor Drug Design
Letters in Drug Design & Discovery Roles of EGFR, PI3K, AKT, and mTOR in Heavy Metal-Induced Cancer
Current Cancer Drug Targets HIV-1 gp120 and Drugs of Abuse: Interactions in the Central Nervous System
Current HIV Research From Multiple PAR1 Receptor/Protein Interactions to their Multiple Therapeutic Implications
Current Topics in Medicinal Chemistry Biological and Clinical Implications of Clonal Heterogeneity and Clonal Evolution in Multiple Myeloma
Current Cancer Therapy Reviews Hedgehog Signaling and Urological Cancers
Current Drug Targets CDK Inhibitors Induce Mitochondria-mediated Apoptosis Through the Activation of Polyamine Catabolic Pathway in LNCaP, DU145 and PC3 Prostate Cancer Cells
Current Pharmaceutical Design The Amyloid β-Protein Precursor and Alzheimers Disease. Therapeutic Approaches
Current Medicinal Chemistry - Central Nervous System Agents Insights into a Critical Role of the FOXO3a-FOXM1 Axis in DNA Damage Response and Genotoxic Drug Resistance
Current Drug Targets