Abstract
Recent progress in understanding the role of catalytically active carbonic anhydrases in tumors has opened new possibilities for diagnostic and/or therapeutic applications of carbonic anhydrase inhibitors selectively blocking the enzyme activity of cancer-related isoforms, namely CA IX and CA XII. Different classes of inhibitors have been investigated in order to evaluate their usefulness as in vivo imaging tools, as modulators of intratumoral pH that influences uptake of conventional chemotherapeutics, or as drugs impeding survival of tumor cells exposed to physiological stresses including hypoxia and acidosis. Here we summarize the most important data related to expression, regulation and functional aspects of cancer-related carbonic anhydrases and discuss advances in synthesis and preclinical studies of isozyme-selective and highly efficient carbonic anhydrase inhibitors.
Keywords: CA VIII isoform, CA9 gene, hypoxia inducible factor 1, tumors, bicarbonate transporters
Current Topics in Medicinal Chemistry
Title: Carbonic Anhydrase Inhibitors and the Management of Cancer
Volume: 7 Issue: 9
Author(s): Silvia Pastorekova, Juraj Kopacek and Jaromir Pastorek
Affiliation:
Keywords: CA VIII isoform, CA9 gene, hypoxia inducible factor 1, tumors, bicarbonate transporters
Abstract: Recent progress in understanding the role of catalytically active carbonic anhydrases in tumors has opened new possibilities for diagnostic and/or therapeutic applications of carbonic anhydrase inhibitors selectively blocking the enzyme activity of cancer-related isoforms, namely CA IX and CA XII. Different classes of inhibitors have been investigated in order to evaluate their usefulness as in vivo imaging tools, as modulators of intratumoral pH that influences uptake of conventional chemotherapeutics, or as drugs impeding survival of tumor cells exposed to physiological stresses including hypoxia and acidosis. Here we summarize the most important data related to expression, regulation and functional aspects of cancer-related carbonic anhydrases and discuss advances in synthesis and preclinical studies of isozyme-selective and highly efficient carbonic anhydrase inhibitors.
Export Options
About this article
Cite this article as:
Pastorekova Silvia, Kopacek Juraj and Pastorek Jaromir, Carbonic Anhydrase Inhibitors and the Management of Cancer, Current Topics in Medicinal Chemistry 2007; 7 (9) . https://dx.doi.org/10.2174/156802607780636708
DOI https://dx.doi.org/10.2174/156802607780636708 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
-
Selective Internal Radiation Therapy with Yttrium-90 for Unresectable Liver Tumours
Reviews on Recent Clinical Trials An Overview of Acute Flaccid Myelitis
CNS & Neurological Disorders - Drug Targets Cell Penetrating Peptides for In Vivo Molecular Imaging Applications
Current Pharmaceutical Design ABC Transporters in Multidrug Resistance and Pharmacokinetics, and Strategies for Drug Development
Current Pharmaceutical Design Pharmacology of TRP Channels in the Vasculature
Current Vascular Pharmacology PET Imaging in Prostate Cancer: Focus on Prostate-Specific Membrane Antigen
Current Topics in Medicinal Chemistry Ribozymes in the Age of Molecular Therapeutics
Current Molecular Medicine Cytochrome P450 2W1 (CYP2W1) in Colorectal Cancers
Current Cancer Drug Targets The Heat Shock Protein 90 Chaperone Complex: An Evolving Therapeutic Target
Current Cancer Drug Targets Polymeric Carriers for Gene Delivery: Chitosan and Poly(amidoamine) Dendrimers
Current Pharmaceutical Design Self-Assembling Peptides: Potential Role in Tumor Targeting
Current Pharmaceutical Biotechnology Interactions of Cisplatin with non-DNA Targets and their Influence on Anticancer Activity and Drug Toxicity: The Complex World of the Platinum Complex
Current Cancer Drug Targets Indoleamine 2,3-Dioxygenase, an Emerging Target for Anti-Cancer Therapy
Current Cancer Drug Targets Epigenetics: Relations to Disease and Laboratory Findings
Current Medicinal Chemistry A Review on Novel Breast Cancer Therapies: Photodynamic Therapy and Plant Derived Agent Induced Cell Death Mechanisms
Anti-Cancer Agents in Medicinal Chemistry Should we Target Allergen Protease Activity to Decrease the Burden of Allergic Airway Inflammation?
Inflammation & Allergy - Drug Targets (Discontinued) Active-Targeted Nanotherapy Strategies for Prostate Cancer
Current Cancer Drug Targets Beyond Cox-Inhibition: ‘Side-Effects’ of Ibuprofen on Neoplastic Development and Progression
Current Pharmaceutical Design Preparation, Characterization, Toxicity and Pharmacodynamics of the Inclusion Complex of Brucea javanica Oil with β-cyclodextrin Polymers
Current Pharmaceutical Biotechnology Challenges in the Correct Assessment of a Case of Aggressive Thyroid Carcinoma with Synchronous Breast Cancer: A Case Report and Review of the Literature of Essential Role of Radiopharmaceuticals
Current Radiopharmaceuticals