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
-
Bio-Distribution, Imaging Protocols and Diagnostic Accuracy of PET with Tracers of Lipogenesis in Imaging Prostate Cancer: a Comparison between 11C-Choline, 18FFluoroethylcholine and 18F-Methylcholine
Current Pharmaceutical Design Substance P: Structure, Function, and Therapeutics
Current Topics in Medicinal Chemistry Genitourinary Tumors: Update on Molecular Biomarkers for Diagnosis, Prognosis and Prediction of Response to Therapy
Current Drug Metabolism Integrins in Drug Targeting-RGD Templates in Toxins
Current Pharmaceutical Design Silencing of Disease-related Genes by Small Interfering RNAs
Current Molecular Medicine Cardiovascular Effects of Current and Future Anti-Obesity Drugs
Current Vascular Pharmacology Beneficial Action of Citrus Flavonoids on Multiple Cancer-Related Biological Pathways
Current Cancer Drug Targets Effect of two Antiandrogens as Protectors of Prostate and Brain in a Huntington`s Animal Model
Anti-Cancer Agents in Medicinal Chemistry Downregulation of CCKBR Expression Inhibits the Proliferation of Gastric Cancer Cells, Revealing a Potential Target for Immunotoxin Therapy
Current Cancer Drug Targets Ocular Inflammatory Diseases: Molecular Pathogenesis and Immunotherapy
Current Molecular Medicine Radiolabelled Oligonucleotides for Imaging of Gene Expression with PET
Current Medicinal Chemistry Anti Cancer Activity on Graviola, an Exciting Medicinal Plant Extract vs Various Cancer Cell Lines and a Detailed Computational Study on its Potent Anti-Cancerous Leads
Current Topics in Medicinal Chemistry The Endothelin Axis: A Novel Target for Pharmacotherapy of Female Malignancies
Current Vascular Pharmacology Serpins for Diagnosis and Therapy in Cancer
Cardiovascular & Hematological Disorders-Drug Targets Imaging of EGFR and EGFR Tyrosine Kinase Overexpression in Tumors by Nuclear Medicine Modalities
Current Pharmaceutical Design Drug Delivery Systems for Chemotherapeutics through Selected Polysaccharidic Vehicles
Current Organic Chemistry <i>In Vivo</i> Anti-Tumor Effects of Flavokawain A in 4T1 Breast Cancer Cell-Challenged Mice
Anti-Cancer Agents in Medicinal Chemistry The Imaging of Apoptosis with the Radiolabelled Annexin A5: A New Tool in Translational Research
Current Clinical Pharmacology New Medical Strategies for Midgut Carcinoids
Anti-Cancer Agents in Medicinal Chemistry Cancer Therapy: Targeting Cell Cycle Regulators
Anti-Cancer Agents in Medicinal Chemistry