Thim L, Hansen M T, Norris K, Hoegh I, Boel E, Forstrom J, Ammerer G, Fiil N P
Proc Natl Acad Sci U S A. 1986 Sep;83(18):6766-70. doi: 10.1073/pnas.83.18.6766.
A series of dibasic insulin precursors including proinsulin was expressed and secreted from Saccharomyces cerevisiae. Recombinant plasmids were constructed to encode fusion proteins consisting of a modified mating factor alpha 1 leader sequence and an insulin precursor. The leader sequence serves to direct the fusion protein into the secretory pathway of the cell and to expose it to the Lys-Arg processing enzyme system. The secreted peptides were purified from the fermentation broth and characterized by sequencing and amino acid analysis. Processing at one or both dibasic sequences was shown in proinsulin and in other insulin precursors containing a short spacer peptide in place of the C peptide. In contrast, no processing was observed in the absence of a spacer peptide in the insulin precursor molecule, e.g., B-Lys-Arg-A (where A and B are the A and B chain of human proinsulin, respectively). This type of single-chain insulin precursors isolated from such constructions could be enzymatically converted into insulin by treatment with trypsin and carboxypeptidase B. The above results suggest that the C-peptide region of proinsulin serves to direct the trypsin-like converting enzyme to process at the two dibasic sequences. We propose that in hormone precursors in general the spacer peptides serve to expose dibasic sequences for processing.
一系列包括胰岛素原在内的二元胰岛素前体在酿酒酵母中得以表达和分泌。构建了重组质粒以编码由修饰的α1交配因子前导序列和胰岛素前体组成的融合蛋白。该前导序列用于将融合蛋白引导至细胞的分泌途径,并使其暴露于赖氨酸-精氨酸加工酶系统。从发酵液中纯化分泌的肽,并通过测序和氨基酸分析进行表征。胰岛素原以及其他含有短间隔肽替代C肽的胰岛素前体在一个或两个二元序列处均发生了加工。相比之下,在胰岛素前体分子中不存在间隔肽的情况下(例如B-赖氨酸-精氨酸-A,其中A和B分别为人胰岛素原的A链和B链),未观察到加工现象。从这类构建体中分离出的这种单链胰岛素前体可通过用胰蛋白酶和羧肽酶B处理而酶促转化为胰岛素。上述结果表明,胰岛素原的C肽区域用于引导类胰蛋白酶转化酶在两个二元序列处进行加工。我们提出,一般而言,在激素前体中,间隔肽用于暴露二元序列以进行加工。