Abstract
N-BP, rapamycin and its derivatives have been originally developed respectively as anti-resorptive and anti-fungal agents. In fact, in vitro and in vivo experiments demonstrated that these compounds are multi-functional molecules exerting their effects on tumour cell growth and bone remodelling. The major challenge in treating cancer relates to mutations in key genes such as p53, Rb or proteins affecting caspase signalling carried by many tumour cells. Whether nitrogen containing bisphosphonates (N-BP) are potent bone inhibitors, they also inhibit tumour cell proliferation and increase atypical apoptosis of bone tumour cells regardless of the p53 and Rb status. N-BP may be then considered as effective therapeutic agents in clinical trials of bone tumours. Rapamycin and its derivatives inhibit mTOR dependent mRNA translation both in osteoclasts and tumour cells. Cellular physiological mechanisms regulated by mTOR integrate many environmental parameters including growth factors, hormones, cytokines, amino acids, energy availability and cellular stresses that are coupled with cell cycle progression and cell growth. Rapamycin and its derivatives as well as N-BP must be considered as bi-(multi) functional molecules affecting simultaneously bone and tumour metabolisms. The present survey describes these two molecular families and discusses their therapeutic interests for primary bone tumours and bone metastases.
Keywords: Rapamycin, bisphosphonate, bone, osteolysis, bone remodelling, primary bone tumours, metastases
Current Medicinal Chemistry
Title: mTOR Inhibitors (Rapamycin and its Derivatives) and Nitrogen Containing Bisphosphonates: Bi-Functional Compounds for the Treatment of Bone Tumours
Volume: 14 Issue: 13
Author(s): Benjamin Ory, Gatien Moriceau, Francoise Redini and Dominique Heymann
Affiliation:
Keywords: Rapamycin, bisphosphonate, bone, osteolysis, bone remodelling, primary bone tumours, metastases
Abstract: N-BP, rapamycin and its derivatives have been originally developed respectively as anti-resorptive and anti-fungal agents. In fact, in vitro and in vivo experiments demonstrated that these compounds are multi-functional molecules exerting their effects on tumour cell growth and bone remodelling. The major challenge in treating cancer relates to mutations in key genes such as p53, Rb or proteins affecting caspase signalling carried by many tumour cells. Whether nitrogen containing bisphosphonates (N-BP) are potent bone inhibitors, they also inhibit tumour cell proliferation and increase atypical apoptosis of bone tumour cells regardless of the p53 and Rb status. N-BP may be then considered as effective therapeutic agents in clinical trials of bone tumours. Rapamycin and its derivatives inhibit mTOR dependent mRNA translation both in osteoclasts and tumour cells. Cellular physiological mechanisms regulated by mTOR integrate many environmental parameters including growth factors, hormones, cytokines, amino acids, energy availability and cellular stresses that are coupled with cell cycle progression and cell growth. Rapamycin and its derivatives as well as N-BP must be considered as bi-(multi) functional molecules affecting simultaneously bone and tumour metabolisms. The present survey describes these two molecular families and discusses their therapeutic interests for primary bone tumours and bone metastases.
Export Options
About this article
Cite this article as:
Ory Benjamin, Moriceau Gatien, Redini Francoise and Heymann Dominique, mTOR Inhibitors (Rapamycin and its Derivatives) and Nitrogen Containing Bisphosphonates: Bi-Functional Compounds for the Treatment of Bone Tumours, Current Medicinal Chemistry 2007; 14 (13) . https://dx.doi.org/10.2174/092986707780831159
DOI https://dx.doi.org/10.2174/092986707780831159 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
Current advances in inherited cardiomyopathy
Describe in detail all novel advances in multimodality imaging related to inherited cardiomyopathy diagnosis and prognosis. Shed light to deeper phenotypic characterization. Acknowledge recent advances in genetics, genomics and precision medicineread 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
-
The Design and Development of Deferiprone (L1) and Other Iron Chelators for Clinical Use: Targeting Methods and Application Prospects
Current Medicinal Chemistry Mutational Analysis of Interleukin-11 and its Consequences on Cancer and COVID-19 Related Cytokine Storm -An Extensive Molecular Dynamics Study
Protein & Peptide Letters Gene Clusters, Molecular Evolution and Disease: A Speculation
Current Genomics Hypertension and Diabetes: Emphasis on the Renin-Angiotensin System in Atherosclerosis
Current Hypertension Reviews Amyloid-Beta Peptide 1-42 Causes Microtubule Deregulation through N-methyl-D-aspartate Receptors in Mature Hippocampal Cultures
Current Alzheimer Research Artificial Blood: A Futuristic Dimension of Modern Day Transfusion Sciences
Cardiovascular & Hematological Agents in Medicinal Chemistry Momordica balsamina: A Medicinal and Neutraceutical Plant for Health Care Management
Current Pharmaceutical Biotechnology Endogenous Opioids and Addiction to Alcohol and other Drugs of Abuse
Current Topics in Medicinal Chemistry Chymase Inhibitor As a Novel Therapeutic Strategy for Anti-Vascular Remodeling
Vascular Disease Prevention (Discontinued) β-sitosterol: Bioactive Compounds in Foods, their Role in Health Promotion and Disease Prevention “A Concise Report of its Phytopharmaceutical Importance”
Current Traditional Medicine Cutaneous Larva Migrans
Recent Patents on Inflammation & Allergy Drug Discovery Electroporation Gene Therapy: New Developments In Vivo and In Vitro
Current Gene Therapy Carotid Artery Disease: Current Concepts on Endothelial Dysfunction and Matrix Remodeling
Current Drug Therapy Gene Therapeutic Approaches for Immune Modulation in AIDS
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Diketo Acids Derivatives as Integrase Inhibitors: The War Against the Acquired Immunodeficiency Syndrome
Recent Patents on Anti-Infective Drug Discovery Non-Analgesic Effects of Opioids: Opioid-induced Respiratory Depression
Current Pharmaceutical Design Pharmacogenetics and Statin Treatment: Reality or Theory?
Current Vascular Pharmacology Patients with Rheumatic Diseases Overlooked during COVID-19 Pandemic: How are They Doing and Behaving?
Current Rheumatology Reviews Risk Factors for Development of Heart Failure
Current Cardiology Reviews Overexpressing Runx2 of BMSCs Improves the Repairment of knee Cartilage Defects
Current Gene Therapy