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
AlphaFold in Medicinal Chemistry: Opportunities and Challenges
AlphaFold, a groundbreaking AI tool for protein structure prediction, is revolutionizing drug discovery. Its near-atomic accuracy unlocks new avenues for designing targeted drugs and performing efficient virtual screening. However, AlphaFold's static predictions lack the dynamic nature of proteins, crucial for understanding drug action. This is especially true for multi-domain proteins, ...read more
Artificial intelligence for Natural Products Discovery and Development
Our approach involves using computational methods to predict the potential therapeutic benefits of natural products by considering factors such as drug structure, targets, and interactions. We also employ multitarget analysis to understand the role of drug targets in disease pathways. We advocate for the use of artificial intelligence in predicting ...read more
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
Chronic Kidney Disease
The scope of the special thematic issue includes but not limited to the mechanism of chronic kidney disease (CKD), the treatment of renal fibrosis and early diagnosis of CKD and so on. We also welcome manuscripts from other scientific research area with respect to internal medicine. Cell death has been ...read more
![](/images/wayfinder.jpg)
- 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
-
The “Entourage Effect”: Terpenes Coupled with Cannabinoids for the Treatment of Mood Disorders and Anxiety Disorders
Current Neuropharmacology Circulating Tumor Cells: A New Window for Diagnosis and Evaluation of Cancer
Anti-Cancer Agents in Medicinal Chemistry Alcoholic/Nonalcoholic Fatty Liver Disease Detection with Transient Elastography: A Detailed Review and Meta-analysis
Current Medical Imaging Contribution of Latin American Countries to Cancer Research and Patent Generation: Recent Patents
Recent Patents on Anti-Cancer Drug Discovery Curcumin in Combined Cancer Therapy
Current Pharmaceutical Design The Role of Leukotrienes Inhibitors in the Management of Chronic Inflammatory Diseases
Recent Patents on Inflammation & Allergy Drug Discovery Dynamic Contrast-Enhanced MRI in Oncology Drug Development
Current Clinical Pharmacology MATra - Magnet Assisted Transfection: Combining Nanotechnology and Magnetic Forces to Improve Intracellular Delivery of Nucleic Acids
Current Pharmaceutical Biotechnology AKT Signaling in Regulating Angiogenesis
Current Cancer Drug Targets Targeting the Tumor Proteasome as a Mechanism to Control the Synthesis and Bioactivity of Matrix Macromolecules
Current Molecular Medicine Targeting Epidermal Growth Factor Receptor in Solid Tumors: Critical Evaluation of the Biological Importance of Therapeutic Monoclonal Antibodies
Current Medicinal Chemistry Current State of the Art of New Tubulin Inhibitors in the Clinic
Current Clinical Pharmacology Antibody Engineering for Targeted Therapy of Cancer Recombinant Fv-Immunotoxins
Current Pharmaceutical Biotechnology Subject Index to Volume 9
Current Pharmaceutical Design Influence of Aldo-keto Reductase 1C3 in Prostate Cancer - A Mini Review
Current Cancer Drug Targets Epigenetic Regulation of Cytochrome P450 Enzymes and Clinical Implication
Current Drug Metabolism Novel Biomarkers for Posterior Urethral Valve
Current Medicinal Chemistry Positron Emission Tomography and Computer Tomography (PET/CT) in Prostate, Bladder, and Testicular Cancers
Current Medicinal Chemistry Phyto-Phospholipid Complexation as a Novel Drug Delivery System for Management of Cancer with Better Bioavailability: Current Perspectives and Future Prospects
Anti-Cancer Agents in Medicinal Chemistry Recurrent Left Atrial Low-grade Malignant Inflammatory Myofibroblastic Tumor Characterized by Cardiovascular Magnetic Resonance
Current Medical Imaging