Henrich Stefan, Lindberg Iris, Bode Wolfram, Than Manuel E
Max-Planck-Institut für Biochemie, Abteilung für Strukturforschung, Am Klopferspitz 18, 82152 Martinsried, Germany.
J Mol Biol. 2005 Jan 14;345(2):211-27. doi: 10.1016/j.jmb.2004.10.050.
In eukaryotes, many secreted proteins and peptide hormones are excised from larger precursors by calcium-dependent serine proteinases, the proprotein/prohormone convertases (PCs). These PCs cleave their protein substrates very specifically following multiple basic residues. The seven mammalian PCs and their yeast orthologue kexin are multi-domain proteinases consisting of a subtilisin-related catalytic domain, a conserved P-domain and a variable, often cysteine-rich domain, which in some PCs is followed by an additional C-terminal trans-membrane domain and a short cytoplasmic domain. The recently published crystal structures of the soluble mouse furin and yeast kexin ectodomains have revealed the relative arrangement of catalytic and P domains, the exact domain fold and the detailed architecture of the substrate binding clefts. Based on these experimental structures, we now have modelled the structures of the other human/mouse PCs. According to topology and to structure-based sequence comparisons, these other PCs closely resemble furin, with PC4, PACE4 and PC5/6 being more similar, and PC1/3, PC2 and PC7 being less similar to furin. Except for PC1 and PC2, this order of similarity is valid for the catalytic as well as for the P domains, and is almost reversed using kexin as a reference molecule. A similar order results from the number and clustering of negative charges lining the non-prime subsites, explaining the gradually decreasing requirement for basic residues N-terminal to substrate cleavage sites. The preference of the different PCs for distinct substrates seems to be governed by overall charge compensation and matching of the detailed charge distribution pattern.
在真核生物中,许多分泌蛋白和肽类激素是由钙依赖性丝氨酸蛋白酶(即前蛋白/前激素转化酶,简称 PCs)从较大的前体中切割出来的。这些 PCs 会在多个碱性残基之后非常特异性地切割其蛋白质底物。七种哺乳动物 PCs 及其酵母同源物凯新是多结构域蛋白酶,由一个枯草杆菌蛋白酶相关催化结构域、一个保守的 P 结构域和一个可变的、通常富含半胱氨酸的结构域组成,在某些 PCs 中,该结构域之后还有一个额外的 C 末端跨膜结构域和一个短的细胞质结构域。最近发表的可溶性小鼠弗林蛋白酶和酵母凯新胞外结构域的晶体结构揭示了催化结构域和 P 结构域的相对排列、确切的结构域折叠以及底物结合裂隙的详细结构。基于这些实验结构,我们现在已经对其他人/小鼠 PCs 的结构进行了建模。根据拓扑结构和基于结构的序列比较,这些其他 PCs 与弗林蛋白酶非常相似,其中 PC4、PACE4 和 PC5/6 更为相似,而 PC1/3、PC2 和 PC7 与弗林蛋白酶的相似性较低。除了 PC1 和 PC2,这种相似性顺序对于催化结构域和 P 结构域都是有效的,并且以凯新作为参考分子时几乎相反。类似的顺序也来自于非主要亚位点内衬负电荷的数量和聚集情况,这解释了底物切割位点 N 端对碱性残基的需求逐渐降低的现象。不同 PCs 对不同底物的偏好似乎由整体电荷补偿和详细电荷分布模式的匹配所决定。