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Current Pharmaceutical Design


ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

Fluorescence- and Spin-Labeled Carbonic Anhydrase Inhibitors

Author(s): Alessandro Cecchi and Claudiu T. Supuran

Volume 14, Issue 7, 2008

Page: [699 - 707] Pages: 9

DOI: 10.2174/138161208783877839

Price: $65


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

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