Tendamistat (HOE 467), a tight-binding α-amylase inhibitor from Streptomyces tendae 4158
Tendamistat (HOE 467), a tight-binding α-amylase inhibitor from Streptomyces tendae 4158
复制标题
Tendamistat (HOE 467)，一种来自 Streptomyces tentae 4158 的紧密结合 α-淀粉酶抑制剂
DOI：
--
复制
发表时间：
1984
期刊：
影响因子：
--
通讯作者：
G. Nesemann
中科院分区：
文献类型：
--
作者：
L. Vértesy;V. Oeding;R. Bender;K. Zepf;G. Nesemann
Streptomyces tentae 4158 (ATCC 31210) 培养液中含有一种新型多肽 α-淀粉酶抑制剂。替达司他（HOE 467）。描述了分离该抑制剂的几种方法，包括两种产生均质材料的快速结晶方法。腾达司他的一个特点是其紧密结合、不依赖于 pH 的抑制动力学以及对哺乳动物 α-淀粉酶的特异性抑制。该抑制剂和 α-淀粉酶形成化学计量 1:1 的复合物，无法通过十二烷基硫酸钠或分子筛色谱法将其分离成单独的组分。作用方式的研究表明，α-淀粉酶抑制活性与抑制剂的完整二硫桥有关。假定酶和tenamistat之间存在多点蛋白质-蛋白质键。结果表明，细胞外的tenamistat抑制链霉菌形成的淀粉酶。因此，我们假设微生物具有调节功能。还描述了具有类似酶抑制特性的泰达司他的副产物。
Culture fluids of Streptomyces tendae 4158 (ATCC 31210) contain a new kind of polypeptide α-amylase inhibitor. tendamistat (HOE 467). Several methods of isolating this inhibitor are described, including two rapid crystallisation methods, which produce homogeneous material. A characteristic of tendamistat is its tight-binding, pH-independent inhibition kinetics and the specific inhibition of the mammalian α-amylases. The inhibitor and the α-amylase form a stoichiometric 1:1 complex, which cannot be separated into its individual components by sodium dodecyl sulphate or molecular sieve chromatography. Studies of the mode of action reveal that the α-amylase-inhibiting activity is linked to the intact disulphide bridges of the inhibitor. It is assumed that the multipoint protein-protein bond exists between the enzyme and tendamistat. It is shown that extracellular tendamistat inhibits amylase formed by streptomyces. We therefore assume a regulatory function in the microorganism. By-products of tendamistat, which possess similar enzyme-inhibiting properties, are also described.