Abstract
Background & Aim: The ubiquitin-proteasome system (UPS) is the major pathway for degrading the intracellular proteins. The 2004 Nobel Prize in Chemistry was awarded to Rose, Hershko, and Ciechanover to highlight the fundamental importance of UPS.
Method & Results: The alterations in this process have been shown to contribute to the cancer progression. Hence, UPS has become a popular target for developing chemotherapeutics against tumours. The application of bortezomib showed high efficiency in treating haematological malignancies by interfering with UPS activity. Many compounds are being screened and evaluated in recent pharmacological advances, either as single agents or in synergy with other drugs, and more to be revealed. Conclusion: In the present review, we exhibit the crucial ingredients involved in UPS and discuss the current situation of small molecules targeting various components of ubiquitination pathway in cancer treatment.Keywords: Ubiquitin, cancer, small molecule inhibitors, proteasome, E3 ligase, deubiquitinating enzyme.
Combinatorial Chemistry & High Throughput Screening
Title:The Small Molecules Targeting Ubiquitin-Proteasome System for Cancer Therapy
Volume: 20 Issue: 5
Author(s): Nannan Ao, Qianping Chen and Geng Liu*
Affiliation:
- School of Radiation Medicine and Protection, Medical College of Soochow University, Collaborative Innovation Center of Radiological Medicine of Jiangsu Higher Education Institutions, Suzhou 215123,China
Keywords: Ubiquitin, cancer, small molecule inhibitors, proteasome, E3 ligase, deubiquitinating enzyme.
Abstract: Background & Aim: The ubiquitin-proteasome system (UPS) is the major pathway for degrading the intracellular proteins. The 2004 Nobel Prize in Chemistry was awarded to Rose, Hershko, and Ciechanover to highlight the fundamental importance of UPS.
Method & Results: The alterations in this process have been shown to contribute to the cancer progression. Hence, UPS has become a popular target for developing chemotherapeutics against tumours. The application of bortezomib showed high efficiency in treating haematological malignancies by interfering with UPS activity. Many compounds are being screened and evaluated in recent pharmacological advances, either as single agents or in synergy with other drugs, and more to be revealed. Conclusion: In the present review, we exhibit the crucial ingredients involved in UPS and discuss the current situation of small molecules targeting various components of ubiquitination pathway in cancer treatment.Export Options
About this article
Cite this article as:
Ao Nannan, Chen Qianping and Liu Geng *, The Small Molecules Targeting Ubiquitin-Proteasome System for Cancer Therapy, Combinatorial Chemistry & High Throughput Screening 2017; 20 (5) . https://dx.doi.org/10.2174/1386207320666170710124746
DOI https://dx.doi.org/10.2174/1386207320666170710124746 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
Call for Papers in Thematic Issues
Artificial Intelligence Methods for Biomedical, Biochemical and Bioinformatics Problems
Recently, a large number of technologies based on artificial intelligence have been developed and applied to solve a diverse range of problems in the areas of biomedical, biochemical and bioinformatics problems. By utilizing powerful computing resources and massive amounts of data, methods based on artificial intelligence can significantly improve the ...read more
Eco-friendly Agents for Biological Control of Pathogenic Diseases
The discovery of an alternative biological approach to disease management includes work on medicinal products derived from natural sources as a starting point for the development of eco-friendly agents for these diseases and the injuries they cause, as well as reducing human contact with hazardous chemicals and their residues. We ...read more
Emerging trends in diseases mechanisms, noble drug targets and therapeutic strategies: focus on immunological and inflammatory disorders
Recently infectious and inflammatory diseases have been a key concern worldwide due to tremendous morbidity and mortality world Wide. Recent, nCOVID-9 pandemic is a good example for the emerging infectious disease outbreak. The world is facing many emerging and re-emerging diseases out breaks at present however, there is huge lack ...read more
Exploring Spectral Graph Theory in Combinatorial Chemistry
Scope of the Thematic Issue: Combinatorial chemistry involves the synthesis and analysis of a large number of diverse compounds simultaneously. Traditional methods rely on brute force experimentation, which can be time-consuming and resource-intensive. Spectral Graph Theory, a branch of mathematics dealing with the properties of graphs in relation to the ...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
-
D1 and Functionally Selective Dopamine Agonists as Neuroprotective Agents in Parkinsons Disease
CNS & Neurological Disorders - Drug Targets Chinese Medicine in Inhalation Therapy: A Review of Clinical Application and Formulation Development
Current Pharmaceutical Design Biomarkers for Early Detection of Colitis-associated Colorectal Cancer - Current Concepts, Future Trends
Current Drug Targets Topical Analgesics in Neuropathic Pain
Current Pharmaceutical Design GCPII Variants, Paralogs and Orthologs
Current Medicinal Chemistry Angiogenesis Inhibition: State of the Art, Forgotten Strategies and New Perspectives in Cancer Therapy
Current Cancer Therapy Reviews Population Pharmacokinetic Evaluation of a Fully Human IgG2 Monoclonal Antibody in Patients with Inflammatory Diseases
Inflammation & Allergy - Drug Targets (Discontinued) Retraction Notice: The Benefits and Risks of Different Therapies in Preventing Postoperative Nausea and Vomiting in Patients Undergoing Thyroid Surgery
Current Drug Safety D-Galactose as a Vector for Prodrug Design
Current Topics in Medicinal Chemistry Nifurtimox Hampered the Progression of Astroglioma <i>In vivo Via</i> Manipulating the AKT-GSK3β axis
Current Molecular Medicine Carotenoids in Photooxidative Stress
Current Nutrition & Food Science Dietary Agents for Prostate Cancer Chemoprevention: An Overview
Current Cancer Therapy Reviews Opportunities for Photoacoustic-Guided Drug Delivery
Current Drug Targets Recent Advances in the Medicinal Chemistry of α-Aminoboronic Acids, Amine-Carboxyboranes and Their Derivatives
Mini-Reviews in Medicinal Chemistry Alpha Fetoprotein is More than a Hepatocellular Cancer Biomarker: From Spontaneous Immune Response in Cancer Patients to the Development of an AFP-Based Cancer Vaccine
Current Molecular Medicine Indoleamine 2,3-dioxygenase (IDO): Biology and Target in Cancer Immunotherapies
Current Cancer Drug Targets Therapeutic Potential of Photochemically Active Metal Complexes based on Interaction with Enzymes
Current Topics in Medicinal Chemistry Study of Monocytes/Macrophages Stimuli as the Targets of Treating Inflammatory Bone Diseases
Current Drug Targets Predictors and Clinical Implications of HPV Reservoire Districts for Genital Tract Disease
Current Pharmaceutical Design Editorial (Thematic Issue: Breast Cancer Clinical Trials – The Era of the Surrogates)
Reviews on Recent Clinical Trials