Bioorganic & Medicinal Chemistry Letters 2006-08-01

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

Seppo Parkkila, Daniela Vullo, Luca Puccetti, Anna-Kaisa Parkkila, Andrea Scozzafava, Claudiu T Supuran

Index: Bioorg. Med. Chem. Lett. 16 , 3955-9, (2006)

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Abstract

The first activation study of isoform XIII of carbonic anhydrase (CA, EC 4.2.1.1) is reported. A series of amino acids and amines incorporating protonatable moieties of the primary/heterocyclic amine type were included in the study. As for CA I and II, CA XIII activators enhance kcat and show no effect on KM, for the physiologic reaction catalyzed by this isoform. Excellent CA XIII activating properties were shown by D-amino acids (His, Phe, DOPA, and Trp), serotonin, and 4-(2-aminoethyl)-morpholine, whereas the corresponding L-amino acids, dopamine, histamine, and 1-(2-aminoethyl)-piperazine, were weaker activators.