Abstract
This review focuses on the recent patents and use of small-molecule inhibitors (SMIs) of Bcl-2 family proteins as therapeutic agents against cancer. Bcl-2 members are crucial regulators of apoptotic cell death. Apoptosis is an evolutionarily conserved process of programmed cell death that plays an essential role in organism development and tissue homeostasis. Several mechanisms exist allowing cells to escape programmed cell death among them is the overexpression of the antiapoptotic proteins. Cancer cells are often found to overexpress many of these members such as Bcl-2, Bcl-XL, Mcl-1, Bcl-w and A1/Bfl1 and are usually resistant to a wide range of anti-cancer drugs and treatments. Many groups have been working to develop anti-cancer drugs that block the function of anti-apoptotic Bcl-2 members, thus favoring cell death. Methods include the downregulation of Bcl-2 expression or the use of peptides or small organic molecules to the Bcl-2 binding pocket, preventing its sequestration of proapoptotic proteins such as Bid and Bim. One of the most promising aspects of SMIs in treating cancer is that their targets and mechanisms of action are different from those of cytotoxic drugs and radiation. This makes it feasible to combine SMIs with other treatments, creating a synergistic therapy, without likely development of cross-resistance or increased toxicity. A broad-spectrum or “pan” SMI which targets multiple Bcl-2 family proteins is the goal.
Keywords: Bcl-2, Bcl-XL, Mcl-1, Bcl-w, A1/Bfl1, therapeutic gents, cancer, Bcl-2 expression
Recent Patents on Anti-Cancer Drug Discovery
Title: Small-Molecule Inhibitors of Bcl-2 Family Proteins as Therapeutic Agents in Cancer
Volume: 3 Issue: 1
Author(s): Ramzi Mohammad, Anshu Giri and Anton-Scott Goustin
Affiliation:
Keywords: Bcl-2, Bcl-XL, Mcl-1, Bcl-w, A1/Bfl1, therapeutic gents, cancer, Bcl-2 expression
Abstract: This review focuses on the recent patents and use of small-molecule inhibitors (SMIs) of Bcl-2 family proteins as therapeutic agents against cancer. Bcl-2 members are crucial regulators of apoptotic cell death. Apoptosis is an evolutionarily conserved process of programmed cell death that plays an essential role in organism development and tissue homeostasis. Several mechanisms exist allowing cells to escape programmed cell death among them is the overexpression of the antiapoptotic proteins. Cancer cells are often found to overexpress many of these members such as Bcl-2, Bcl-XL, Mcl-1, Bcl-w and A1/Bfl1 and are usually resistant to a wide range of anti-cancer drugs and treatments. Many groups have been working to develop anti-cancer drugs that block the function of anti-apoptotic Bcl-2 members, thus favoring cell death. Methods include the downregulation of Bcl-2 expression or the use of peptides or small organic molecules to the Bcl-2 binding pocket, preventing its sequestration of proapoptotic proteins such as Bid and Bim. One of the most promising aspects of SMIs in treating cancer is that their targets and mechanisms of action are different from those of cytotoxic drugs and radiation. This makes it feasible to combine SMIs with other treatments, creating a synergistic therapy, without likely development of cross-resistance or increased toxicity. A broad-spectrum or “pan” SMI which targets multiple Bcl-2 family proteins is the goal.
Export Options
About this article
Cite this article as:
Mohammad Ramzi, Giri Anshu and Goustin Anton-Scott, Small-Molecule Inhibitors of Bcl-2 Family Proteins as Therapeutic Agents in Cancer, Recent Patents on Anti-Cancer Drug Discovery 2008; 3 (1) . https://dx.doi.org/10.2174/157489208783478676
DOI https://dx.doi.org/10.2174/157489208783478676 |
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
-
The Challenge of microRNA as a Biomarker of Epilepsy
Current Neuropharmacology Recent Progress in Biomedical Applications of Magnetic Nanoparticles
Recent Patents on Nanotechnology C-Met Inhibitors are Potential Novel Therapeutic Agents Against Listeria monocytogenes Infection Through Blocking the Bacteria Entry into Nonphagocytic Cells
Current Topics in Medicinal Chemistry Irreversible LSD1 Inhibitors: Application of Tranylcypromine and Its Derivatives in Cancer Treatment
Current Topics in Medicinal Chemistry Editorial (Thematic Issue: New Therapeutic Approaches for the Treatment of Glioblastoma)
Current Cancer Drug Targets Bioconversion of Isoflavones into Bioactive Equol: State of the Art
Recent Patents on Food, Nutrition & Agriculture Dietary Fatty Acids in Metabolic Syndrome, Diabetes and Cardiovascular Diseases
Current Diabetes Reviews MicroRNA-490-5P Targets CCND1 to Suppress Cellular Proliferation in Glioma Cells and Tissue Through Cell Cycle Arrest
Current Neurovascular Research Establishment of Cholinergic Neuron-like Cell Lines with Differential Vulnerability to Nitrosative Stress
Current Neurovascular Research Rotundic Acid Regulates the Effects of Let-7f-5p on Caco2 Cell Proliferation
Anti-Cancer Agents in Medicinal Chemistry Emerging Role of Circular RNAs in Kidney Diseases in Nephrology
Current Drug Targets Sunlight Vitamin D and Skin Cancer
Anti-Cancer Agents in Medicinal Chemistry Targeting Tumor Proteasome with Traditional Chinese Medicine
Current Drug Discovery Technologies [18F]Fluoroalkyl Agents: Synthesis, Reactivity and Application for Development of PET Ligands in Molecular Imaging
Current Topics in Medicinal Chemistry Anti-inflammatory and Immune Therapy for Alzheimers Disease: Current Status and Future Directions
Current Neuropharmacology Emerging Roles for Modulation of microRNA Signatures in Cancer Chemoprevention
Current Cancer Drug Targets Focal Adhesion Kinase as a Cancer Therapy Target
Anti-Cancer Agents in Medicinal Chemistry Quinazolines as Apoptosis Inducers and Inhibitors: A Review of Patent Literature
Recent Patents on Anti-Cancer Drug Discovery An Appraisal of Current Pharmacological Perspectives of Sesamol: A Review
Mini-Reviews in Medicinal Chemistry Application of NMR to the Study of Cells and Body Fluids
Current Organic Chemistry