Abstract
Alkylating agents such as temozolomide (TMZ) are effective anticancer drugs for treating a variety of solid tumors including melanoma, glioma, and astrocytoma. TMZ exerts its effects mainly via the mutagenic product O6-methylguanine, a cytotoxic DNA lesion. This damage may be repaired by the DNA repair enzyme O6-methylguanine DNA methyltransferase (MGMT), a key player in the resistance of cancers to TMZ. Several strategies are presently being pursued to improve the killing of tumor cells by TMZ, with inhibition of MGMT being the most promising. In this review, we provide an overview of recent advances in this field.
Keywords: Temozolomide, DNA repair, MGMT, cancer therapy, Alkylating agents, anticancer drugs, solid tumors, melanoma, glioma, astrocytoma
Current Medicinal Chemistry
Title:Strategies to Improve the Killing of Tumors Using Temozolomide: Targeting the DNA Repair Protein MGMT
Volume: 19 Issue: 23
Author(s): G. Jiang, L. -T. Li, Y. Xin, L. Zhang, Y. -Q. Liu and J. -N. Zheng
Affiliation:
Keywords: Temozolomide, DNA repair, MGMT, cancer therapy, Alkylating agents, anticancer drugs, solid tumors, melanoma, glioma, astrocytoma
Abstract: Alkylating agents such as temozolomide (TMZ) are effective anticancer drugs for treating a variety of solid tumors including melanoma, glioma, and astrocytoma. TMZ exerts its effects mainly via the mutagenic product O6-methylguanine, a cytotoxic DNA lesion. This damage may be repaired by the DNA repair enzyme O6-methylguanine DNA methyltransferase (MGMT), a key player in the resistance of cancers to TMZ. Several strategies are presently being pursued to improve the killing of tumor cells by TMZ, with inhibition of MGMT being the most promising. In this review, we provide an overview of recent advances in this field.
Export Options
About this article
Cite this article as:
Jiang G., -T. Li L., Xin Y., Zhang L., -Q. Liu Y. and -N. Zheng J., Strategies to Improve the Killing of Tumors Using Temozolomide: Targeting the DNA Repair Protein MGMT, Current Medicinal Chemistry 2012; 19 (23) . https://dx.doi.org/10.2174/092986712802002446
DOI https://dx.doi.org/10.2174/092986712802002446 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
- 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
-
ZIP4 is a Novel Diagnostic and Prognostic Marker in Human Pancreatic Cancer: A Systemic Comparison Between EUS-FNA and Surgical Specimens
Current Molecular Medicine 3-Carboranyl Thymidine Analogues (3CTAs) and Other Boronated Nucleosides for Boron Neutron Capture Therapy
Anti-Cancer Agents in Medicinal Chemistry Organoselenium Compounds in Cancer Chemoprevention
Mini-Reviews in Medicinal Chemistry Protein Degradation by the Ubiquitin-Proteasome Pathway and Organ Fibrosis
Current Medicinal Chemistry Targeting the Epidermal Growth Factor Pathway as Therapy for Glioblastoma
Current Cancer Therapy Reviews Targeting Nodal and Cripto-1: Perspectives Inside Dual Potential Theranostic Cancer Biomarkers
Current Medicinal Chemistry Diverse Models for the Prediction of Dual mTOR and PI3Kα Inhibitory Activities of Substituted 4-morpholinopyrrolopyrimidines
Letters in Drug Design & Discovery Dibenzofurans from Lichens – A Pharmacological Overview
Current Topics in Medicinal Chemistry Molecular Mechanisms Regulating the Mitochondrial Targeting of Microsomal Cytochrome P450 EnzymesMolecular Mechanisms Regulating the Mitochondrial Targeting of Microsomal Cytochrome P450 Enzymes
Current Drug Metabolism Phenylbutyric Acid: Simple Structure - Multiple Effects
Current Pharmaceutical Design Nanocrystals: From Raw Material to the Final Formulated Oral Dosage Form - A Review
Current Pharmaceutical Design Difluorinated Curcumin: A Promising Curcumin Analogue with Improved Anti-Tumor Activity and Pharmacokinetic Profile
Current Pharmaceutical Design Metabolism and Pharmacological Mechanisms of Active Ingredients in <i>Erigeron breviscapus</i>
Current Drug Metabolism Suicide Gene Therapy Mediated by the Herpes Simplex Virus Thymidine Kinase Gene / Ganciclovir System: Fifteen Years of Application
Current Gene Therapy Molecular Imaging of Stem Cell Transplantation for Neurodegenerative Diseases
Current Pharmaceutical Design Novel Marine-Derived Anti-Cancer Agents
Current Pharmaceutical Design Therapeutic Potential of Metabotropic Glutamate Receptor Modulators
Current Neuropharmacology 5'-Nucleotidases, Nucleosides and their Distribution in the Brain: Pathological and Therapeutic Implications
Current Medicinal Chemistry New Perspectives in Glioblastoma: Nanoparticles-based Approaches
Current Cancer Drug Targets The Use of Herbal Medicine in Cancer-related Anorexia/ Cachexia Treatment Around the World
Current Pharmaceutical Design