Abstract
Aberrant activation of the PI3K/Akt/mTOR pathway is found in many types of cancer and thus plays a major role in breast cancer cell proliferation and anti-cancer drug resistance. The mechanisms involved in the activation of this pathway include: constitutively activated receptor tyrosine kinases (IGF/IGFR, ErbB, FGF/FGFR systems) leading to constitutive activation of PI3K; loss of PTEN function; PI3K mutations; aberrant activation of Akt, eIF4E, 4E-BP1 and p70S6K. These alterations trigger a cascade of biological events, from cell growth and proliferation to survival and migration, which contribute to tumor progression. Therefore, the PI3K/Akt/mTOR pathway is considered an attractive target for the development of novel anti-cancer molecules, and several specific tyrosine kinase inhibitors and signal transduction inhibitors specifically targeting the kinases involved in this pathway have been developed. Many of these inhibitors currently under clinical evaluation represent a promising approach for the treatment of breast cancer patients. This review provides an overview of the most recent patents, of pre-clinical and clinical studies of inhibitors targeting the different members and/or activators of the PI3K/Akt/mTOR pathway, used alone or in combination with other targeted agents for the treatment of breast cancer.
Keywords: Breast cancer, PI3K/Akt/mTOR pathway, PI3K inhibitors, Akt inhibitors, mTOR inhibitors, tyrosine kinase inhibitors, combination therapies, pre-clinical studies, clinical trials, patents
Recent Patents on Anti-Cancer Drug Discovery
Title: Inhibitors of the PI3K/Akt/mTOR Pathway: New Hope for Breast Cancer Patients
Volume: 5 Issue: 1
Author(s): Sandra E. Ghayad and Pascale A. Cohen
Affiliation:
Keywords: Breast cancer, PI3K/Akt/mTOR pathway, PI3K inhibitors, Akt inhibitors, mTOR inhibitors, tyrosine kinase inhibitors, combination therapies, pre-clinical studies, clinical trials, patents
Abstract: Aberrant activation of the PI3K/Akt/mTOR pathway is found in many types of cancer and thus plays a major role in breast cancer cell proliferation and anti-cancer drug resistance. The mechanisms involved in the activation of this pathway include: constitutively activated receptor tyrosine kinases (IGF/IGFR, ErbB, FGF/FGFR systems) leading to constitutive activation of PI3K; loss of PTEN function; PI3K mutations; aberrant activation of Akt, eIF4E, 4E-BP1 and p70S6K. These alterations trigger a cascade of biological events, from cell growth and proliferation to survival and migration, which contribute to tumor progression. Therefore, the PI3K/Akt/mTOR pathway is considered an attractive target for the development of novel anti-cancer molecules, and several specific tyrosine kinase inhibitors and signal transduction inhibitors specifically targeting the kinases involved in this pathway have been developed. Many of these inhibitors currently under clinical evaluation represent a promising approach for the treatment of breast cancer patients. This review provides an overview of the most recent patents, of pre-clinical and clinical studies of inhibitors targeting the different members and/or activators of the PI3K/Akt/mTOR pathway, used alone or in combination with other targeted agents for the treatment of breast cancer.
Export Options
About this article
Cite this article as:
Ghayad E. Sandra and Cohen A. Pascale, Inhibitors of the PI3K/Akt/mTOR Pathway: New Hope for Breast Cancer Patients, Recent Patents on Anti-Cancer Drug Discovery 2010; 5 (1) . https://dx.doi.org/10.2174/157489210789702208
DOI https://dx.doi.org/10.2174/157489210789702208 |
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
-
Structure and Expression of Different Serum Amyloid A (SAA) Variants and their Concentration-Dependent Functions During Host Insults
Current Medicinal Chemistry Epigenetic Regulation of Epithelial to Mesenchymal Transition
Current Cancer Drug Targets Ghrelin: A Gastric Peptide that Regulates Hypothalamic Control of Feeding
Current Medicinal Chemistry - Central Nervous System Agents Aloperine Induces Apoptosis by a Reactive Oxygen Species Activation Mechanism in Human Ovarian Cancer Cells
Protein & Peptide Letters The Significance of Transferrin Receptors in Oncology: the Development of Functional Nano-based Drug Delivery Systems
Current Drug Delivery Insulin-Like Growth Factor 1 Receptor Targeted Therapeutics: Novel Compounds and Novel Treatment Strategies for Cancer Medicine
Recent Patents on Anti-Cancer Drug Discovery Computational Approaches for the Identification and Optimization of Src Family Kinases Inhibitors
Current Medicinal Chemistry Targeted Delivery of Colloidal Silver for MCF-7 Breast Cancer Treatment
Current Drug Delivery Clinical Pharmacogenetics in Oncology: the Paradigm of Molecular Targeted Therapies
Current Pharmaceutical Design Phytochemical-Mediated Glioma Targeted Treatment: Drug Resistance and Novel Delivery Systems
Current Medicinal Chemistry Patent Selections:
Recent Patents on Anti-Cancer Drug Discovery ADAM28 as a Target for Human Cancers
Current Pharmaceutical Design New Insights in Drug-Induced Mitochondrial Toxicity
Current Pharmaceutical Design Chemically Functionalized Carbon Nanotubes: Emerging Vectors for Cell Therapy
Mini-Reviews in Medicinal Chemistry Overlapping Ligand Specificity of P-Glycoprotein and Serum α1-Acid Glycoprotein:Evidences and Potential Implications
Current Drug Metabolism Recent Advances in Superparamagnetic Iron Oxide Based Nanoprobes as Multifunctional Theranostic Agents for Breast Cancer Imaging and Therapy
Current Medicinal Chemistry The Toll-Like Receptor Radical Cycle Pathway: A New Drug Target in Immune-Related Chronic Fatigue
CNS & Neurological Disorders - Drug Targets Etiology of Neuroinflammatory Pathologies in Neurodegenerative Diseases: A Treatise
Current Psychopharmacology Rational Design and Development of Colon-Specific Prodrugs
Current Topics in Medicinal Chemistry The Safety of the Temozolomide in Patients with Malignant Glioma
Current Drug Safety