Abstract
Carbonic anhydrase IX (hCA IX) is a membrane-associated glycoprotein that is observed in many tumor tissues and is strongly overexpressed by hypoxia conditions. Hypoxia is a clinically important tumor parameter and this enzyme can play an important role as a potential marker of hypoxic tumor and as a therapeutic target too. In the last years, Carbonic Anhydrase IX Inhibitors which possess fluorescent probe were largely used for visualize hypoxic tumor cell lines and for understanding the biological roles of hCA IX in acidification of the external matrix. Here we resume the developement pathways of such compounds from the design to the final biological evaluation. Furthermore, spin-labeled CAIs were included to have a complete overview of the potenciality of this enzyme as marker of hypoxic tumors.
Keywords: Carbonic anhydrase inhibitors, hCA IX, hypoxic tumor, extracellular pH, fluorescent sulfonamide, spin-labeled sulfonamide
Current Pharmaceutical Design
Title: Fluorescence- and Spin-Labeled Carbonic Anhydrase Inhibitors
Volume: 14 Issue: 7
Author(s): Alessandro Cecchi and Claudiu T. Supuran
Affiliation:
Keywords: Carbonic anhydrase inhibitors, hCA IX, hypoxic tumor, extracellular pH, fluorescent sulfonamide, spin-labeled sulfonamide
Abstract: Carbonic anhydrase IX (hCA IX) is a membrane-associated glycoprotein that is observed in many tumor tissues and is strongly overexpressed by hypoxia conditions. Hypoxia is a clinically important tumor parameter and this enzyme can play an important role as a potential marker of hypoxic tumor and as a therapeutic target too. In the last years, Carbonic Anhydrase IX Inhibitors which possess fluorescent probe were largely used for visualize hypoxic tumor cell lines and for understanding the biological roles of hCA IX in acidification of the external matrix. Here we resume the developement pathways of such compounds from the design to the final biological evaluation. Furthermore, spin-labeled CAIs were included to have a complete overview of the potenciality of this enzyme as marker of hypoxic tumors.
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Cite this article as:
Cecchi Alessandro and Supuran T. Claudiu, Fluorescence- and Spin-Labeled Carbonic Anhydrase Inhibitors, Current Pharmaceutical Design 2008; 14 (7) . https://dx.doi.org/10.2174/138161208783877839
DOI https://dx.doi.org/10.2174/138161208783877839 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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