Abstract
Aberrations in the Ubiquitin-Proteasome System (UPS) have been recently connected to the pathogenesis of several human protein degradation disorders (e.g., cancer and neurodegenerative diseases), so that proteasome is now considered an important target for drug discovery. Small molecules able to inhibit and modulate UPS have been, in fact, described as novel tools for a new approach in anti-cancer therapy. In particular Proteasome Inhibitors (PIs), blocking activation of nuclear factor-kappa B (NF-kB), trigger a decreased cellular proliferation and angiogenic cytokine production, induce cell death and inhibit tumor cell adhesion to stroma. Furthermore, several studies have demonstrated that PIs potentiate the activity of other anti-cancer treatment, in part by down-regulating chemoresistance pathways. Therefore pharmacologic, preclinical, and clinical data suggested the use of PIs in anticancer strategies, for their potential therapeutic relevance in the treatment of cancer and inflammatory-related diseases. This review focuses on recent advances in the development of PIs anticancer agents highlighting both novel patented compounds and novel therapeutic protocol of intervention.
Keywords: Proteasome Inhibitors (PIs), protein degradation disorders, cancer
Recent Patents on Anti-Cancer Drug Discovery
Title: Proteasome Inhibitors Therapeutic Strategies for Cancer
Volume: 4 Issue: 1
Author(s): Annamaria D'Alessandro, Luisa Pieroni, Maurizio Ronci, Simona D'Aguanno, Giorgio Federici and Andrea Urbani
Affiliation:
Keywords: Proteasome Inhibitors (PIs), protein degradation disorders, cancer
Abstract: Aberrations in the Ubiquitin-Proteasome System (UPS) have been recently connected to the pathogenesis of several human protein degradation disorders (e.g., cancer and neurodegenerative diseases), so that proteasome is now considered an important target for drug discovery. Small molecules able to inhibit and modulate UPS have been, in fact, described as novel tools for a new approach in anti-cancer therapy. In particular Proteasome Inhibitors (PIs), blocking activation of nuclear factor-kappa B (NF-kB), trigger a decreased cellular proliferation and angiogenic cytokine production, induce cell death and inhibit tumor cell adhesion to stroma. Furthermore, several studies have demonstrated that PIs potentiate the activity of other anti-cancer treatment, in part by down-regulating chemoresistance pathways. Therefore pharmacologic, preclinical, and clinical data suggested the use of PIs in anticancer strategies, for their potential therapeutic relevance in the treatment of cancer and inflammatory-related diseases. This review focuses on recent advances in the development of PIs anticancer agents highlighting both novel patented compounds and novel therapeutic protocol of intervention.
Export Options
About this article
Cite this article as:
D'Alessandro Annamaria, Pieroni Luisa, Ronci Maurizio, D'Aguanno Simona, Federici Giorgio and Urbani Andrea, Proteasome Inhibitors Therapeutic Strategies for Cancer, Recent Patents on Anti-Cancer Drug Discovery 2009; 4 (1) . https://dx.doi.org/10.2174/157489209787002452
DOI https://dx.doi.org/10.2174/157489209787002452 |
Print ISSN 1574-8928 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-3970 |
Call for Papers in Thematic Issues
Novel anti-cancer drugs in photoimmunotherapy management: from bench to translational research
In recent years, traditional cancer treatments, such as surgery, chemotherapy, and radiation treatment, etc., may damage the pathological tissue and normal cells. The ideal tumor treatment should be noninvasive, eliminating the primary tumor, making the body produce systemic tumor-specific immunity, eliminating metastases, and having less /no side effects. Recent Patents ...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
-
Prostate Cancer, miRNAs, Metallothioneins and Resistance to Cytostatic Drugs
Current Medicinal Chemistry Conventional Anticancer Therapeutics and Telomere Maintenance Mechanisms
Current Pharmaceutical Design Targeting Cancer Stem Cells with Repurposed Drugs to Improve Current Therapies
Recent Patents on Anti-Cancer Drug Discovery Subject Index To Volume 4
Cardiovascular & Hematological Agents in Medicinal Chemistry MicroRNAs in the Intracellular Space, Regulation of Organelle Specific Pathways in Health and Disease
MicroRNA Natural Compounds as Anticancer Agents Targeting DNA Topoisomerases
Current Genomics Drug Treatment of Obesity: Established and Emerging Therapies
Mini-Reviews in Medicinal Chemistry Small Molecule Inhibitors of Protein Kinases in Cancer- How to Overcome Resistance
Mini-Reviews in Medicinal Chemistry New Tubulin Polymerization Inhibitor Derived from Thalidomide: Implications for Anti-Myeloma Therapy
Current Medicinal Chemistry Vasoproliferation and Antiproliferative Treatment Options in Pulmonary Arterial Hypertension
Recent Patents on Cardiovascular Drug Discovery Role of microRNAs in Chronic Lymphocytic Leukemia Pathogenesis
Current Medicinal Chemistry Unravelling the Role of Infectious Agents in the Pathogenesis of Human Autoimmunity: The Hypothesis of the Retroviral Involvement Revisited
Current Molecular Medicine Is Going for Cure in CML Targeting Aberrant Glycogen Synthase Kinase 3β?
Current Drug Targets STAT-3 Inhibitors: State of the Art and New Horizons for Cancer Treatment
Current Medicinal Chemistry Drug Targeting Strategies in Cancer Treatment: An Overview
Mini-Reviews in Medicinal Chemistry Defining and Managing Expectations for Early Immunotherapy Cancer Trials
Reviews on Recent Clinical Trials Tumor Necrosis Factor-α-Mediated Pulmonary Endothelial Barrier Dysfunction
Current Respiratory Medicine Reviews The Role of the Tyrosine Kinase Inhibitor STI571 in the Treatment of Cancer
Current Cancer Drug Targets Target Acquired: Progress and Promise of Targeted Therapeutics in the Treatment of Prostate Cancer
Current Cancer Drug Targets Need to Think Outside Organ-based Diagnosis to Molecular Diagnostics
Applied Clinical Research, Clinical Trials and Regulatory Affairs