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首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Activation studies of the β-carbonic anhydrases from Malassezia restricta with amines and amino acids
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Activation studies of the β-carbonic anhydrases from Malassezia restricta with amines and amino acids

机译:用胺和氨基酸的Malassezia Restrictaβ-碳酸酐酶的活化研究

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The β-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 (KsubA/sub of 15?nM), 2-aminoethyl-piperazine/morpholine (KsubA/subs of 0.25–0.33?μM), histamine, L-4-amino-phenylalanine, D-Phe, L-/D-DOPA, and L-/D-Trp (KsubA/subs of 0.32???0.90?μM). 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?μM. 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.
机译:最近克隆和表征的机会理性病原体Malassezia Restricta(MRCCA)基因组的β-碳酸酐酶(Ca,EC 4.2.1.1)已经研究了胺和氨基酸面板的酶活化。在本研究中测试的24种化合物中,最有效的MRCCA活化剂是L-肾上腺素(K 为15·nm),2-氨基乙基 - 哌嗪/吗啉(K a S的0.25-0.33Ωμm),组胺,L-4-氨基 - 苯丙氨酸,D-PHE,L- / D-DOPA和L- / D-TRP(k a s 0.32 ??? 0.90?μm)。最低有效的活化剂是L- / D-Tyr,L-ASP,L- / D-Glu和L-HI,其活化常数在4.04和12.8Ωμm之间。由于MRCA涉及头皮屑和Seborrhoeic皮炎,这些结果旨在鉴定参与此类真菌的代谢过程的酶活性的调节剂。

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