Carbonic Anhydrase Activation and the Drug Design

Author(s): Claudia Temperini, Andrea Scozzafava, Claudiu T. Supuran.

Journal Name: Current Pharmaceutical Design

Volume 14 , Issue 7 , 2008

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Abstract:

The activation mechanism of Carbonic Anhydrase was recently explained using kinetic, spectroscopic and X-ray techniques. It has been demonstrated that the activators molecules (CAAs) bind at the entrance of the enzyme active-site facilitating the ratedetermining step of CA catalitic cycle. Drug design studies have been performed in order to obtain strong CAAs belonging to several chemical classes: amino acids, azoles, amine and their derivatives, etc. Structure-activity correlations of different activators are discussed for the most studied Carbonic Anhydrase isozymes: isoform I and II. The physiological relevance of CA activation and the possible application of CAAs in Alzheimers desease and for other memory therapies are also treated.

Keywords: Carbonic anhydrase, X-ray structure, kinetic, enzyme activator, Alzheimer's desease

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Article Details

VOLUME: 14
ISSUE: 7
Year: 2008
Page: [708 - 715]
Pages: 8
DOI: 10.2174/138161208783877857
Price: $58

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