Literature

Abstract

An activation study of the human carbonic anhydrase (hCA, EC 4.2.1.1) isozymes VII 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 microM). 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 microM). 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.

DOI： 10.1016/j.bmcl.2007.05.052

Carbonic anhydrase activators: Activation of the human isoforms VII (cytosolic) and XIV (transmembrane) with amino acids and amines

Bioorganic & Medicinal Chemistry Letters 2007.0

Carbonic anhydrase activators: Activation of the human cytosolic isozyme III and membrane-associated isoform IV with amino acids and amines

Bioorganic & Medicinal Chemistry Letters 2008.0

Carbonic anhydrase activators. Activation of the membrane-associated isoform XV with amino acids and amines

Bioorganic & Medicinal Chemistry Letters 2009.0

Carbonic anhydrase activators: Activation of the human tumor-associated isozymes IX and XII with amino acids and amines

Bioorganic & Medicinal Chemistry 2008.0

Carbonic anhydrase activators: Activation of isozyme XIII with amino acids and amines

Bioorganic & Medicinal Chemistry Letters 2006.0

Carbonic anhydrase activators: The first activation study of the human secretory isoform VI with amino acids and amines