Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 15, Pages 4107-4112Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.05.052
Keywords
carbonic anhydrase; activator; proton transfer; amine; amino acid; Alzheimer's disease
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An activation study of the human carbonic anhydrase (hCA, EC 4.2.1.1) isozymes VI I and XIV using a small library of natural/non-natural amino acids and aromatic/heterocyclic amines is reported. hCA VII was efficiently activated by L-/D-His, dopamine and serotonin (K(A)s of 0.71-0.93 mu M). The best hCA XIV activators were histamine (K-A of 10 nM), L-Phe, L-/D-His and 4-amino-L-Phe (K(A)s of 0,24-2.90 mu M). In view of the significant expression levels of CA VII and CA XIV in the brain, selective activation of these isoforms may be useful when developing pharmacologic agents for the management of major disorders such as epilepsy and Alzheimer's disease. (c) 2007 Elsevier Ltd. All rights reserved.
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