Carbonic anhydrase activators: Activation of the β-carbonic anhydrase from Malassezia globosa with amines and amino acids

Bioorganic & Medicinal Chemistry Letters
2016.0

Abstract

The β-carbonic anhydrase (CA, EC 4.2.1.1) from the dandruff producing fungus Malassezia globosa, MgCA, was investigated for its activation with amines and amino acids. MgCA was weakly activated by amino acids such as L-/D-His, L-Phe, D-DOPA, D-Trp, L-/D-Tyr and by the amine serotonin (KAs of 12.5-29.3μM) but more effectively activated by d-Phe, l-DOPA, l-Trp, histamine, dopamine, pyridyl-alkylamines, and 4-(2-aminoethyl)-morpholine, with KAs of 5.82-10.9μM. The best activators were l-adrenaline and 1-(2-aminoethyl)piperazine, with activation constants of 0.72-0.81μM. This study may help a better understanding of the activation mechanisms of β-CAs from pathogenic fungi as well as the design of tighter binding ligands for this enzyme which is a drug target for novel types of anti-dandruff agents.

Knowledge Graph

Similar Paper

Carbonic anhydrase activators: Activation of the β-carbonic anhydrase from Malassezia globosa with amines and amino acids
Bioorganic & Medicinal Chemistry Letters 2016.0
Carbonic anhydrase activators: Activation of the β-carbonic anhydrase from the pathogenic yeast Candida glabrata with amines and amino acids
Bioorganic & Medicinal Chemistry Letters 2010.0
Carbonic anhydrase activators: Activation of the β-carbonic anhydrase Nce103 from the yeast Saccharomyces cerevisiae with amines and amino acids
Bioorganic & Medicinal Chemistry Letters 2009.0
Carbonic anhydrase activators: Activation of the β-carbonic anhydrases from the pathogenic fungi Candida albicans and Cryptococcus neoformans with amines and amino acids
Bioorganic & Medicinal Chemistry 2010.0
Molecular Cloning, Characterization, and Inhibition Studies of a β-Carbonic Anhydrase from Malassezia globosa, a Potential Antidandruff Target
Journal of Medicinal Chemistry 2012.0
Dithiocarbamates effectively inhibit the β-carbonic anhydrase from the dandruff-producing fungus Malassezia globosa
Bioorganic & Medicinal Chemistry 2017.0
Activation studies with amines and amino acids of the α-carbonic anhydrase from the pathogenic protozoan Trypanosoma cruzi
Bioorganic & Medicinal Chemistry 2018.0
Carbonic anhydrase activators: Activation of the archaeal β-class (Cab) and γ-class (Cam) carbonic anhydrases with amino acids and amines
Bioorganic & Medicinal Chemistry Letters 2008.0
Carbonic anhydrase activators: Activation of isozyme XIII with amino acids and amines
Bioorganic & Medicinal Chemistry Letters 2006.0
Inhibition of Malassezia globosa carbonic anhydrase with phenols
Bioorganic & Medicinal Chemistry 2017.0