Abstract
Carbonic anhydrase IX (CA IX) is a tumor associated protein, since it is highly expressed in a multitude of carcinomas, while it is present in a limited number of normal tissues. It is a multi-domain protein consisting of an N-terminal proteoglycan-like (PG) domain, a catalytic domain, a trans-membrane portion (TM) and an intracytoplasmatic (IC) segment. These domains have peculiar biochemical and physiological features. Among these, only the PG domain is unique among the CA family. This review focuses on the most recent molecular and catalytic features uncovered of this enzyme, the role of its different domains in tumor physiology, and its three dimensional structure which has recently been solved. In addition, we present recent advances in the development of antibodies and small inhibiting molecules able to target CA IX for diagnostic and therapeutic applications.
Keywords: Anti-tumor drugs, carbonic anhydrase IX, inhibitors, monoclonal antibody, structure based drug design, Carbonic anhydrase, tumor, intracytoplasmatic, enzyme, carcinomas
Current Medicinal Chemistry
Title: Carbonic Anhydrase IX as a Target for Designing Novel Anticancer Drugs
Volume: 19 Issue: 6
Author(s): S. M. Monti, C. T. Supuran and G. De Simone
Affiliation:
Keywords: Anti-tumor drugs, carbonic anhydrase IX, inhibitors, monoclonal antibody, structure based drug design, Carbonic anhydrase, tumor, intracytoplasmatic, enzyme, carcinomas
Abstract: Carbonic anhydrase IX (CA IX) is a tumor associated protein, since it is highly expressed in a multitude of carcinomas, while it is present in a limited number of normal tissues. It is a multi-domain protein consisting of an N-terminal proteoglycan-like (PG) domain, a catalytic domain, a trans-membrane portion (TM) and an intracytoplasmatic (IC) segment. These domains have peculiar biochemical and physiological features. Among these, only the PG domain is unique among the CA family. This review focuses on the most recent molecular and catalytic features uncovered of this enzyme, the role of its different domains in tumor physiology, and its three dimensional structure which has recently been solved. In addition, we present recent advances in the development of antibodies and small inhibiting molecules able to target CA IX for diagnostic and therapeutic applications.
Export Options
About this article
Cite this article as:
M. Monti S., T. Supuran C. and De Simone G., Carbonic Anhydrase IX as a Target for Designing Novel Anticancer Drugs, Current Medicinal Chemistry 2012; 19 (6) . https://dx.doi.org/10.2174/092986712799034851
DOI https://dx.doi.org/10.2174/092986712799034851 |
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
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...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
- 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
-
Metallothioneins and Cancer
Current Protein & Peptide Science Tannic Acid Inhibits Proliferation, Migration, Invasion of Prostate Cancer and Modulates Drug Metabolizing and Antioxidant Enzymes
Anti-Cancer Agents in Medicinal Chemistry The Effects of Cantharidin and Cantharidin Derivates on Tumour Cells
Anti-Cancer Agents in Medicinal Chemistry Editorial [Clinical Applications of Advanced CT, MRI and Optical Imagings as Well as Spect]
Current Medical Imaging Toll-Like Receptors in Alzheimer's Disease: A Therapeutic Perspective
CNS & Neurological Disorders - Drug Targets Copper Complexes as Anticancer Agents
Anti-Cancer Agents in Medicinal Chemistry Gynaecological Cancer Diagnostics: 99mTc-Cisplatin Complex as a Future Approach for Early, Prompt and Efficient Diagnosis of Gynaecological Cancer
Current Medical Imaging Innovations and Improvements in Pharmacokinetic Models Based on Physiology
Current Drug Delivery Novel Oral Anticoagulants: Recommendations for Patient Evaluation, Treatment Initiation, Follow-up and Perioperative Management
Cardiovascular & Hematological Disorders-Drug Targets DLEU2: A Meaningful Long Noncoding RNA in Oncogenesis
Current Pharmaceutical Design The Yin and Yang of microRNA Assay Methods
MicroRNA Medical Treatment of Overactive Bladder: An Overview
Current Clinical Pharmacology DNA Binding Mode of Transition Metal Complexes, A Relationship to Tumor Cell Toxicity
Current Medicinal Chemistry The Pim Kinases: New Targets for Drug Development
Current Drug Targets Applications of 211At and 223Ra in Targeted Alpha-Particle Radiotherapy
Current Radiopharmaceuticals FRET Based Ratio-Metric Sensing of Hyaluronidase in Synthetic Urine as a Biomarker for Bladder and Prostate Cancer
Current Pharmaceutical Biotechnology Dual Time F-18 FDG PET/CT Imaging in the Diagnosis of Renal Cell Cancer
Current Medical Imaging Paclitaxel Formulations: Challenges and Novel Delivery Options
Current Drug Delivery Transition Metal-Based Prodrugs for Anticancer Drug Delivery
Current Medicinal Chemistry ABC Pumps and Their Role in Active Drug Transport
Current Topics in Medicinal Chemistry