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
![](/images/wayfinder.jpg)
- 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
-
A Novel H.264-Supported Approach for Detecting and Classifying Hepatic Lesions in Computed Tomographic Images
Current Medical Imaging Prostaglandin E2 Receptors as Potential Bone Anabolic Targets – Selective EP4 Receptor Agonists
Current Molecular Pharmacology Pharmacogenomic Approaches for Tailored Anti-Leukemic Therapy in Children
Current Medicinal Chemistry The Role of Androgen Receptor Mutations in Prostate Cancer Progression
Current Genomics 15,16-dihydrotanshinone I Induces Apoptosis and Inhibits the Proliferation, Migration of Human Osteosarcoma Cell Line 143B in vitro
Anti-Cancer Agents in Medicinal Chemistry Characterization of the Lymphotropic Amplicons-6 and Tamplicon-7 Vectors Derived from HHV-6 and HHV-7
Current Gene Therapy Biocompatible Europium Doped Hydroxyapatite Nanoparticles as a Biological Fluorescent Probe
Current Nanoscience CXCR4-targeted Nanoparticles Reduce Cell Viability, Induce Apoptosis and Inhibit SDF-1α Induced BT-549-Luc Cell Migration In Vitro
Current Drug Delivery Anti-Angiogenic Therapies in the Treatment of Waldenstrom's Macroglobulinemia
Current Cancer Drug Targets Proteases as Anti-Cancer Targets - Molecular and Biological Basis for Development of Inhibitor-Like Drugs Against Cancer
Anti-Cancer Agents in Medicinal Chemistry Neuropilin Signalling in Vascular Development and Pathology
Current Angiogenesis (Discontinued) Treatment Strategy Issues for Chronic HIV-1 Infection in Adults: The Dilemma of Life-long Antiretroviral Treatment
Current Medicinal Chemistry - Anti-Infective Agents Experimental Strategies in Autoimmunity: Antagonists of Cytokines and their Receptors, Nanocarriers, Inhibitors of Immunoproteasome, Leukocyte Migration and Protein Kinases
Current Pharmaceutical Design Design, Synthesis and Molecular Modeling Studies of Some Heterocyclic Compounds Derived from the Suzuki-coupling of 6-bromo-1,3,4-oxadiazine Together with their Antitumor and Anti-leishmanial Evaluations
Current Organic Chemistry Anti-Biofilm Strategies and the Need for Innovations in Wound Care
Recent Patents on Anti-Infective Drug Discovery CEBP Epigenetic Dysregulation as a Drug Target for the Treatment of Hematologic and Gynecologic Malignancies
Current Drug Targets The Correlation between EGFR and Androgen Receptor Pathways: A Novel Potential Prognostic Marker in Gastric Cancer
Anti-Cancer Agents in Medicinal Chemistry Synthesis and Cytotoxic Evaluation of Novel Symmetrical Taspine Derivatives as Anticancer Agents
Medicinal Chemistry Circulating microRNAs as Potential Diagnostic, Prognostic and Therapeutic Targets in Pancreatic Cancer
Current Pharmaceutical Design Management of Ovarian Cancer in Elderly
Reviews on Recent Clinical Trials