Bioorganic & Medicinal Chemistry Letters 2009-01-01

Carbonic anhydrase activators: Activation of the β-carbonic anhydrase Nce103 from the yeastSaccharomyces cerevisiaewith amines and amino acids

Semra Isik, Feray Kockar, Meltem Aydin, Oktay Arslan, Ozen Ozensoy Guler, Alessio Innocenti, Andrea Scozzafava, Claudiu T. Supuran, Semra Isik, Feray Kockar, Meltem Aydin, Oktay Arslan, Ozen Ozensoy Guler, Alessio Innocenti, Andrea Scozzafava, Claudiu T. Supuran

文献索引：Bioorg. Med. Chem. Lett. 19 , 1662-5, (2009)

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摘要

The protein encoded by the Nce103 gene of Saccharomyces cerevisiae, a beta-carbonic anhydrase (CA, EC 4.2.1.1) designated as scCA, was investigated for its activation with amines and amino acids. scCA was poorly activated by amino acids such as l-/d-His, Phe, DOPA, Trp (K(A)s of 82-90 microM) and more effectively activated by amines such as histamine, dopamine, serotonin, pyridyl-alkylamines, aminoethyl-piperazine/morpholine (K(A)s of 10.2-21.3 microM). The best activator was l-adrenaline, with an activation constant of 0.95 microM. This study may help to better understand the catalytic/activation mechanisms of the beta-CAs and eventually to design modulators of CA activity for similar enzymes present in pathogenic fungi, such as Candida albicans and Cryptococcus neoformans.