Activation studies of the β-carbonic anhydrases from Malassezia restricta with amines and amino acids

被引：3

作者：

Angeli, Andrea ^{[1
]}

Prete, Sonia Del ^{[2
]}

Ghobril, Cynthia ^{[3
]}

Hitce, Julien ^{[3
]}

Clavaud, Cecile ^{[3
]}

Marrat, Xavier ^{[3
]}

Donald, William A. ^{[4
]}

Capasso, Clemente ^{[2
]}

Supuran, Claudiu T. ^{[1
,4
]}

机构：

[1] Univ Firenze, Dipartimento Neurofarba, Sez Sci Farmaceut & Nutraceut, Via U Schiff 6, I-50019 Sesto Fiorentino, Florence, Italy

[2] CNR, Inst Biosci & Bioresources, Dept Biol Agr & Food Sci, Via Pietro Castellino 111, I-80131 Naples, Italy

[3] LOreal Res & Innovat, Aulnay Sous Bois, France

[4] Univ New South Wales, Sch Chem, Sydney, NSW, Australia

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2020年 / 35卷 / 01期

基金：

澳大利亚研究理事会;

关键词：

Carbonic anhydrase; activator; beta-class enzyme; pathogenic fungi; amine; amino acid; BIOLOGICAL EVALUATION; ISOZYME-II; SPECTROSCOPIC INVESTIGATIONS; PLASMODIUM-FALCIPARUM; PATHOGENIC BACTERIA; SCHIFF-BASES; IX; VII; INHIBITION; DISCOVERY;

D O I：

10.1080/14756366.2020.1743284

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The beta-carbonic anhydrase (CA, EC 4.2.1.1) from the genome of the opportunistic pathogen Malassezia restricta (MreCA), which was recently cloned and characterised, herein has been investigated for enzymatic activation by a panel of amines and amino acids. Of the 24 compounds tested in this study, the most effective MreCA activators were L-adrenaline (K-A of 15 nM), 2-aminoethyl-piperazine/morpholine (K(A)s of 0.25-0.33 mu M), histamine, L-4-amino-phenylalanine, D-Phe, L-/D-DOPA, and L-/D-Trp (K(A)s of 0.32 - 0.90 mu M). The least effective activators were L-/D-Tyr, L-Asp, L-/D-Glu, and L-His, with activation constants ranging between 4.04 and 12.8 mu M. As MreCA is involved in dandruff and seborrhoeic dermatitis, these results are of interest to identify modulators of the activity of enzymes involved in the metabolic processes of such fungi.

引用

页码：824 / 830

页数：7

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