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.
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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 |
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