Abstract
Telomerase is a ribonucleoprotein polymerase that maintains the length of telomeric DNA by adding hexameric units (TTAGGG) to the ends of the chromosomes. This mechanism prevents replicative senescence, thus conferring unlimited proliferative potential to cells. Telomerase reactivation has been detected in most human tumour tissue, indicating that the enzyme may be useful as a specific tumour marker. The inhibition of telomerase causes a progressive and critical reduction of telomeres, leading to a potent signal for the blockage of cell proliferation and the induction of apoptosis. Since normal somatic cells lack telomerase activity, the anti-telomerase approach is highly specific for tumour cells and metastases. Prolonged treatment is required before enzyme deactivation causes the telomeres to be shortened enough to induce senescence and apoptosis. Therefore, the drugs employed in anti-telomerase therapy should be of only moderate non-specific cytotoxicity. Certain cis-Pt(II)-complexes have recently been shown to be effective inhibitors of telomerase in both cell-free and in vitro assays, most likely by targeting the nucleobases of the RNA component of the enzyme.
Keywords: Telomerase, telomere, antiproliferative agents, platinum(II) complexes
Current Medicinal Chemistry
Title: Telomerase Inhibition and Cancer: Might Platinum Based Drugs have a Future as Anti-telomerase Pharmacological Approach?
Volume: 12 Issue: 26
Author(s): Donato Colangelo and Domenico Osella
Affiliation:
Keywords: Telomerase, telomere, antiproliferative agents, platinum(II) complexes
Abstract: Telomerase is a ribonucleoprotein polymerase that maintains the length of telomeric DNA by adding hexameric units (TTAGGG) to the ends of the chromosomes. This mechanism prevents replicative senescence, thus conferring unlimited proliferative potential to cells. Telomerase reactivation has been detected in most human tumour tissue, indicating that the enzyme may be useful as a specific tumour marker. The inhibition of telomerase causes a progressive and critical reduction of telomeres, leading to a potent signal for the blockage of cell proliferation and the induction of apoptosis. Since normal somatic cells lack telomerase activity, the anti-telomerase approach is highly specific for tumour cells and metastases. Prolonged treatment is required before enzyme deactivation causes the telomeres to be shortened enough to induce senescence and apoptosis. Therefore, the drugs employed in anti-telomerase therapy should be of only moderate non-specific cytotoxicity. Certain cis-Pt(II)-complexes have recently been shown to be effective inhibitors of telomerase in both cell-free and in vitro assays, most likely by targeting the nucleobases of the RNA component of the enzyme.
Export Options
About this article
Cite this article as:
Colangelo Donato and Osella Domenico, Telomerase Inhibition and Cancer: Might Platinum Based Drugs have a Future as Anti-telomerase Pharmacological Approach?, Current Medicinal Chemistry 2005; 12 (26) . https://dx.doi.org/10.2174/092986705774933416
DOI https://dx.doi.org/10.2174/092986705774933416 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
![](/images/wayfinder.jpg)
- Author Guidelines
- Bentham Author Support Services (BASS)
- 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
-
An Update of Radiolabeled Bombesin Analogs for Gastrin-Releasing Peptide Receptor Targeting
Current Pharmaceutical Design Brain Injury Associated with Widely Abused Amphetamines: Neuroinflammation, Neurogenesis and Blood-Brain Barrier
Current Drug Abuse Reviews Lymphangiogenesis and Anti-Tumor Immune Responses
Current Molecular Medicine Antioxidant and Cytotoxicity Activity of Phenolic Compounds from Piper sarmentosum Roxb. Against T47D Human Breast Cancer Cell
The Natural Products Journal Protection and Restitution of Gut Barrier by Probiotics: Nutritional and Clinical Implications
Current Nutrition & Food Science Protective Role of Natural Products in Glioblastoma Multiforme: A Focus on Nitric Oxide Pathway
Current Medicinal Chemistry In Vitro Antitumoral Activity of Palladium(II) and Platinum(II) Complexes with O,O'-Dialkyl Esters of Ethylene-bis(S)-Leucine
Letters in Drug Design & Discovery Hypoxic Regulation of Metastasis via Hypoxia-Inducible Factors
Current Molecular Medicine Multicenter Randomized Controlled Trial for the Treatment of Ulcerative Colitis with a Leukocytapheresis Column
Current Pharmaceutical Design Current Technological Development of Antibody Therapeutics
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Prospects of Bacteriotherapy with Nanotechnology in Nanoparticledrug Conjugation Approach for Cancer Therapy
Current Medicinal Chemistry Polyethyleneimine-Based Nanocarriers for Gene Delivery
Current Pharmaceutical Design Vitamin, Mineral, and Drug Absorption Following Bariatric Surgery
Current Drug Metabolism Lysophosphatidic Acid and Renal Fibrosis
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery (Discontinued) Mesenchymal Stromal Cells; Role in Tissue Repair, Drug Discovery and Immune Modulation
Current Drug Delivery Pharmacological Drug Delivery Strategies for Improved Therapeutic Effects: Recent Advances
Current Pharmaceutical Design Scope of Nanotechnology-based Radiation Therapy and Thermotherapy Methods in Cancer Treatment
Current Cancer Drug Targets Discovery and Development of Natural Products and their Derivatives as Photosensitizers for Photodynamic Therapy
Current Medicinal Chemistry Basic and Clinical Research Against Advanced Glycation End Products (AGEs): New Compounds to Tackle Cardiovascular Disease and Diabetic Complications
Recent Advances in Cardiovascular Drug Discovery (Discontinued) The Antiangiogenic and Antitumoral Activity of Titanocene Y* In Vivo
Letters in Drug Design & Discovery