期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 15, 页码 4107-4112出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.05.052
关键词
carbonic anhydrase; activator; proton transfer; amine; amino acid; Alzheimer's disease
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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