title: Carbonic anhydrase activators: Activation of the β-carbonic anhydrase from Malassezia globosa with amines and amino acids.
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.
authors: Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy.
authors: Daniela
authors: D
authors: Vullo
authors: Istituto di Biochimica delle Proteine-CNR, Via P. Castellino 111, 80131 Napoli, Italy; Università degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino (Florence), Italy.
authors: Sonia
authors: S
authors: Del Prete
authors: Istituto di Biochimica delle Proteine-CNR, Via P. Castellino 111, 80131 Napoli, Italy. Electronic address: clemente.capasso@ibbr.cnr.it.
authors: Clemente
authors: C
authors: Capasso
authors: Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy; Università degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino (Florence), Italy. Electronic address: claudiu.supuran@unifi.it.
authors: Claudiu T
authors: CT
authors: Supuran
mesh_terms: D000588:Amines / Q000494:pharmacology*; D000596:Amino Acids / Q000494:pharmacology*; D000935:Antifungal Agents / Q000494:pharmacology; D002256:Carbonic Anhydrases / Q000378:metabolism*; D063807:Dandruff / Q000188:drug therapy / Q000382:microbiology; D004305:Dose-Response Relationship, Drug; D008024:Ligands; D008290:Malassezia / Q000187:drug effects / Q000201:enzymology*; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000588:Amines; D000596:Amino Acids; D000935:Antifungal Agents; D008024:Ligands; D002256:Carbonic Anhydrases
keywords: Activator; Amine; Amino acid; Carbonic anhydrase; Dandruff; Malassezia globosa