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[借助混合酸酐和酶的蛋白质半合成:胰岛素的化学与合成]

[Protein semisynthesis with the help of mixed anhydrides and enzymes: chemistry and synthesis of insulins].

作者信息

Zahn H, Naithani V K, Gattner H G, Büllesbach E E, Thamm P M

出版信息

Naturwissenschaften. 1981 Feb;68(2):56-62. doi: 10.1007/BF01047223.

Abstract

Proteins play a prominent role in nature and their biosynthesis occurs via stepwise combination of amino acids. One can imitate this method in laboratory or synthesize the polypeptide chain by combining smaller preformed fragments (fragment condensation). Reversible protection of reactive groups and solubility problems arising are the most important features in this regard. Semisynthesis, i.e., coupling of amino acids or peptides to natural material may help to overcome these difficulties. The preparation of hybrid preproinsulin by mixed anhydride synthesis and the conversion of pork insulin to human insulin by enzyme-catalyzed peptide synthesis are two examples of the semisynthesis of proteins. In both cases optimal reaction conditions are essential for maximal yield of the product desired. In spite of the rapid improvement of gene technology, chemical peptide synthesis will retain its value for the preparation of biologically and pharmacologically interesting substances.

摘要

蛋白质在自然界中起着重要作用,其生物合成是通过氨基酸的逐步组合进行的。人们可以在实验室中模仿这种方法,或者通过组合较小的预制片段(片段缩合)来合成多肽链。反应基团的可逆保护以及由此产生的溶解性问题是这方面最重要的特征。半合成,即氨基酸或肽与天然物质的偶联,可能有助于克服这些困难。通过混合酸酐合成制备杂交前胰岛素原以及通过酶催化肽合成将猪胰岛素转化为人胰岛素是蛋白质半合成的两个例子。在这两种情况下,最佳反应条件对于所需产物的最大产率至关重要。尽管基因技术迅速发展,但化学肽合成在制备具有生物学和药理学意义的物质方面仍将保持其价值。

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