Carbonic anhydrase activators: Activation of the β-carbonic anhydrase from the pathogenic yeast Candida glabrata with amines and amino acids
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- 作者：Alessio Innocenti ; Worraanong Leewattanapasuk ; Gheorghe Manole ; Andrea Scozzafava ; Fritz A. Mü ; hlschlegel ; Claudiu T. Supuran
- 关键词：Carbonic anhydrase ; Candida glabrata ; Activator ; Amino acid ; Amine
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2010
- 出版时间：1 March 2010
- 年：2010
- 卷：20
- 期：5
- 页码：1701-1704
- 全文大小：216 K
文摘
The protein encoded by the NCE103 gene of Candida glabrata, a β-carbonic anhydrase (CA, EC 4.2.1.1) designated as CgCA, was investigated for its activation with amines and amino acids. CgCA was weakly activated by amino acids such as l-/d-His, l-Phe, l-DOPA, and l-Trp and by histamine or dopamine (KAs of 21.2–37 μM) but more effectively activated by d-Phe, d-DOPA, d-Trp as well as serotonin, pyridyl-alkylamines, aminoethyl-piperazine/morpholine (KAs of 10.1–16.7 μM). The best activators were l-/d-Tyr, with activation constants of 7.1–9.5 μM. This study may bring a better understanding of the catalytic/activation mechanisms of β-CAs from pathogenic fungi.