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地中海红珊瑚(Corallium rubrum)骨架形成相关的α-碳酸酐酶 CruCA4 的激活谱分析。

Activation Profile Analysis of CruCA4, an α-Carbonic Anhydrase Involved in Skeleton Formation of the Mediterranean Red Coral, Corallium rubrum.

机构信息

Istituto di Bioscienze e Biorisorse, CNR, Via Pietro Castellino 111, 80131 Napoli, Italy.

Dipartimento Di Chimica, Laboratorio di Chimica Bioinorganica, Università degli Studi di Firenze, Polo Scientifico, Via della Lastruccia 3, 50019 Sesto Fiorentino (Florence), Italy.

出版信息

Molecules. 2017 Dec 28;23(1):66. doi: 10.3390/molecules23010066.

Abstract

CruCA4, a coral α-carbonic anhydrase (CA, EC 4.2.1.1) involved in the biomineralization process of the Mediterranean red coral, , was investigated for its activation with a panel of amino acids and amines. Most compounds showed considerable activating properties, with a rather well defined structure-activity relationship. The most effective CruCA4 activators were d-His, 4-H₂N-l-Phe, Histamine, Dopamine, Serotonin, 1-(2-Aminoethyl)-piperazine, and l-Adrenaline, with activation constants in the range of 8-98 nM. Other amines and amino acids, such as d-DOPA, l-Tyr, 2-Pyridyl-methylamine, 2-(2-Aminoethyl) pyridine and 4-(2-Aminoethyl)-morpholine, were submicromolar CruCA4 activators, with K ranging between 0.15 and 0.93 µM. Since it has been shown that CA activators may facilitate the initial phases of in-bone mineralization, our study may be relevant for finding modulators of enzyme activity, which can enhance the formation of the red coral skeleton.

摘要

研究了参与地中海红珊瑚生物矿化过程的珊瑚 α-碳酸酐酶(CA,EC 4.2.1.1)CruCA4 与一系列氨基酸和胺的激活作用。大多数化合物表现出相当大的激活特性,具有相当明确的结构-活性关系。最有效的 CruCA4 激活剂是 d-His、4-H₂N-l-Phe、组氨酸、多巴胺、血清素、1-(2-氨基乙基)-哌嗪和 l-肾上腺素,其激活常数在 8-98 nM 范围内。其他胺和氨基酸,如 d-DOPA、l-Tyr、2-吡啶基甲胺、2-(2-氨基乙基)吡啶和 4-(2-氨基乙基)-吗啉,是 CruCA4 的亚微摩尔激活剂,K 值在 0.15 和 0.93 μM 之间。由于已经表明 CA 激活剂可以促进骨内矿化的初始阶段,因此我们的研究可能与寻找酶活性调节剂有关,这可以增强红珊瑚骨架的形成。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db1c/6017236/b20fb357171c/molecules-23-00066-g001a.jpg

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