The beta-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 (K(A)s of 12.5-29.3 mu M) but more effectively activated by D-Phe, L-DOPA, L-Trp, histamine, dopamine, pyridyl-alkylamines, and 4-(2-aminoethyl)-morpholine, with K(A)s of 5.82-10.9 mu M. The best activators were L-adrenaline and 1-(2-aminoethyl)piperazine, with activation constants of 0.72-0.81 mu M. This study may help a better understanding of the activation mechanisms of beta-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. (C) 2016 Elsevier Ltd. All rights reserved.
Carbonic anhydrase activators: Activation of the beta-carbonic anhydrase from Malassezia globosa with amines and amino acids
Del Prete Sonia;Capasso Clemente;
2016
Abstract
The beta-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 (K(A)s of 12.5-29.3 mu M) but more effectively activated by D-Phe, L-DOPA, L-Trp, histamine, dopamine, pyridyl-alkylamines, and 4-(2-aminoethyl)-morpholine, with K(A)s of 5.82-10.9 mu M. The best activators were L-adrenaline and 1-(2-aminoethyl)piperazine, with activation constants of 0.72-0.81 mu M. This study may help a better understanding of the activation mechanisms of beta-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. (C) 2016 Elsevier Ltd. All rights reserved.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
