Dipartimento Neurofarba, Sezione di Scienze Farmaceutiche e Nutraceutiche, Università degli Studi di Firenze, Sesto Fiorentino (Florence), Italy.
Department of Biology, Agriculture and Food Sciences, Institute of Biosciences and Bioresources, CNR, Napoli, Italy.
J Enzyme Inhib Med Chem. 2020 Dec;35(1):824-830. doi: 10.1080/14756366.2020.1743284.
The β-carbonic anhydrase (CA, EC 4.2.1.1) from the genome of the opportunistic pathogen (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 of 15 nM), 2-aminoethyl-piperazine/morpholine (Ks of 0.25-0.33 µM), histamine, L-4-amino-phenylalanine, D-Phe, L-/D-DOPA, and L-/D-Trp (Ks 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.
β-碳酸酐酶（CA，EC 4.2.1.1）来自机会性病原体（MreCA）的基因组，最近已被克隆和鉴定，本文研究了一组胺和氨基酸对其酶活性的激活作用。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（K 为 15nM）、2-氨基乙基哌嗪/吗啉（Ks 为 0.25-0.33μM）、组氨酸、L-4-氨基苯丙氨酸、D-Phe、L-/D-DOPA 和 L-/D-Trp（Ks 为 0.32-0.90μM）。最无效的激活剂是 L-/D-Tyr、L-Asp、L-/D-Glu 和 L-His，其激活常数在 4.04 到 12.8μM 之间。由于 MreCA 参与头皮屑和脂溢性皮炎，这些结果对于鉴定参与这些真菌代谢过程的酶的活性调节剂具有重要意义。
