Abstract
Regulator of a vast array of vital cellular processes including cell-cycle progression, apoptosis and antigen presentation, the proteasome represents a major therapeutic target. Therefore, selective inhibitors of the proteasome are promising candidates to develop new treatments for diseases like inflammation, immune diseases and cancer. For proof, the boronic acid, Bortezomib has been approved for treating incurable multiple myeloma in 2003 and mantle lymphoma in 2006 and five others proteasome inhibitors are currently in clinical trials for treatment of different cancers. These compounds and many described proteasome inhibitors interact covalently with the active site of the enzyme through an electrophilic reactive function. Non-covalent inhibitors, mainly peptides, pseudopeptides and some organic compounds, have been less widely investigated. Devoid of reactive function prone to nucleophilic attack, they could offer the advantage of an improved selectivity, a less excessive reactivity and instability which are often associated with side effects in therapeutics. This review highlights the current state of research in the field of non-covalent proteasome inhibitors.
Keywords: Proteasome, anti-cancer drugs, non-covalent inhibitors, natural peptides, pseudopeptides, small synthetic molecules.
Current Pharmaceutical Design
Title:Non-Covalent Proteasome Inhibitors
Volume: 19 Issue: 22
Author(s): Julia Kaffy, Guillaume Bernadat and Sandrine Ongeri
Affiliation:
Keywords: Proteasome, anti-cancer drugs, non-covalent inhibitors, natural peptides, pseudopeptides, small synthetic molecules.
Abstract: Regulator of a vast array of vital cellular processes including cell-cycle progression, apoptosis and antigen presentation, the proteasome represents a major therapeutic target. Therefore, selective inhibitors of the proteasome are promising candidates to develop new treatments for diseases like inflammation, immune diseases and cancer. For proof, the boronic acid, Bortezomib has been approved for treating incurable multiple myeloma in 2003 and mantle lymphoma in 2006 and five others proteasome inhibitors are currently in clinical trials for treatment of different cancers. These compounds and many described proteasome inhibitors interact covalently with the active site of the enzyme through an electrophilic reactive function. Non-covalent inhibitors, mainly peptides, pseudopeptides and some organic compounds, have been less widely investigated. Devoid of reactive function prone to nucleophilic attack, they could offer the advantage of an improved selectivity, a less excessive reactivity and instability which are often associated with side effects in therapeutics. This review highlights the current state of research in the field of non-covalent proteasome inhibitors.
Export Options
About this article
Cite this article as:
Kaffy Julia, Bernadat Guillaume and Ongeri Sandrine, Non-Covalent Proteasome Inhibitors, Current Pharmaceutical Design 2013; 19 (22) . https://dx.doi.org/10.2174/1381612811319220016
DOI https://dx.doi.org/10.2174/1381612811319220016 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
- Announcements
Related Articles
-
Hemangiomas, Angiosarcomas, and Vascular Malformations Represent the Signaling Abnormalities of Pathogenic Angiogenesis
Current Molecular Medicine Emergence of Lipid-Based Vesicular Carriers as Nanoscale Pharmacotherapy in Rheumatoid Arthritis
Recent Patents on Nanomedicine Importance of P-gp PET Imaging in Pharmacology
Current Pharmaceutical Design Recent Advances in the Development of Selective Mcl-1 Inhibitors for the Treatment of Cancer (2017-Present)
Recent Patents on Anti-Cancer Drug Discovery Multifaceted Role of Neuropilins in Cancer
Current Medicinal Chemistry Sphere Formation Assay is not an Effective Method for Cancer Stem Cell Derivation and Characterization from the Caco-2 Colorectal Cell Line
Current Stem Cell Research & Therapy Transferrin and the Transferrin Receptor: Of Magic Bullets and Other Concerns
Inflammation & Allergy - Drug Targets (Discontinued) Exploration of Structure-Based on Imidazole Core as Antibacterial Agents
Current Topics in Medicinal Chemistry Subject index to volume 3
Current Molecular Medicine Gene Therapy for Pituitary Tumors
Current Gene Therapy Heteroaromatic Pim Kinase Inhibitors Containing a Pyrazole Moiety
Recent Patents on Anti-Cancer Drug Discovery Synthesis and Preliminary Anti-HIV Activities of Andrographolide Derivatives
Medicinal Chemistry Origins and Consequences of AID Expression in Lymphoid Neoplasms
Current Immunology Reviews (Discontinued) IO Nation: The Rise of Immuno-Oncology
Current Pharmacogenomics and Personalized Medicine Bisphosphonate Therapy in the Treatment of Multiple Myeloma
Current Pharmaceutical Design Structural Insight of NICD-MAML Interactions: Virtual Screening, Docking and Molecular Dynamics Study for Identification of Potential Inhibitor
Letters in Drug Design & Discovery Immune Mechanism, Aging, Season and Diseases: Modulatory Role of Melatonin
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Flavonoids: A Review of Its Commercial Application Potential as Anti- Infective Agents
Current Medicinal Chemistry - Anti-Infective Agents Recent Advances in Molecular Image-Guided Cancer Radionuclide Therapy
Current Drug Targets Intravenous Immunoglobulin as a Potential Therapy for Refractory Urticaria - A Review
Inflammation & Allergy - Drug Targets (Discontinued)