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Activation studies of the β-carbonic anhydrases from Malassezia restricta with amines and amino acids.
Journal of Enzyme inhibition and Medicinal Chemistry ( IF 5.6 ) Pub Date : 2020-03-27 , DOI: 10.1080/14756366.2020.1743284
Andrea Angeli 1 , Sonia Del Prete 2 , Cynthia Ghobril 3 , Julien Hitce 3 , Cécile Clavaud 3 , Xavier Marrat 3 , William A Donald 4 , Clemente Capasso 2 , Claudiu T Supuran 1, 4
Affiliation  

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 (KA of 15 nM), 2-aminoethyl-piperazine/morpholine (KAs of 0.25-0.33 µM), histamine, L-4-amino-phenylalanine, D-Phe, L-/D-DOPA, and L-/D-Trp (KAs 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.

中文翻译:

用胺和氨基酸激活限制马拉色菌的 β-碳酸酐酶。

来自机会性病原体马拉色菌 (MreCA) 基因组的 β-碳酸酐酶 (CA、EC 4.2.1.1) 最近被克隆和表征,本文研究了一组胺和氨基酸的酶促激活情况。在本研究中测试的 24 种化合物中,最有效的 MreCA 激活剂是 L-肾上腺素(KA 为 15 nM)、2-氨基乙基哌嗪/吗啉(KA 为 0.25-0.33 µM)、组胺、L-4-氨基苯丙氨酸、D-Phe、L-/D-DOPA 和 L-/D-Trp(KA 为 0.32 - 0.90 µM)。最无效的激活剂是 L-/D-Tyr、L-Asp、L-/D-Glu 和 L-His,激活常数范围在 4.04 至 12.8 µM 之间。由于 MreCA 与头皮屑和脂溢性皮炎有关,因此这些结果对于鉴定参与此类真菌代谢过程的酶活性调节剂很有意义。
更新日期:2020-04-20
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