Carroll M C, Fathallah D M, Bergamaschini L, Alicot E M, Isenman D E
Department of Pathology, Harvard Medical School, Boston, MA.
Proc Natl Acad Sci U S A. 1990 Sep;87(17):6868-72. doi: 10.1073/pnas.87.17.6868.
The C4B isotype of the fourth component of human complement (C4) displays 3- to 4-fold greater hemolytic activity than does its other isotype C4A. This correlates with differences in their covalent binding efficiencies to erythrocytes coated with antibody and complement C1. C4A binds to a greater extent when C1 is on IgG immune aggregates. The differences in covalent binding properties correlate only with amino acid changes between residues 1101 and 1106 (pro-C4 numbering)--namely, Pro-1101, Cys-1102, Leu-1105, and Asp-1106 in C4A and Leu-1101, Ser-1102, Ile-1105, and His-1106 in C4B, which are located in the C4d region of the alpha chain. To more precisely identify the residues that are important for the functional differences, C4A-C4B hybrid proteins were constructed by using recombinant DNA techniques. Comparison of these by hemolytic assay and binding to IgG aggregates showed that the single substitution of aspartic acid for histidine at position 1106 largely accounted for the change in functional activity and nature of the chemical bond formed (ester vs. amide). Surprisingly, substitution of a neutral residue, alanine, for histidine at position 1106 resulted in an increase in binding to immune aggregates without subsequent reduction in the hemolytic activity. This result strongly suggests that position 1106 is not "catalytic" as previously proposed but interacts sterically/electrostatically with potential acceptor sites and serves to "select" binding sites on potential acceptor molecules.
人类补体第四成分(C4)的C4B同种型比其另一种同种型C4A表现出高3至4倍的溶血活性。这与其与包被抗体和补体C1的红细胞的共价结合效率差异相关。当C1存在于IgG免疫聚集体上时,C4A的结合程度更高。共价结合特性的差异仅与1101至1106位残基(前C4编号)之间的氨基酸变化相关,即C4A中的Pro-1101、Cys-1102、Leu-以及C4B中的Leu-1101、Ser-1102、Ile-1105和His-1106,这些位于α链的C4d区域。为了更精确地鉴定对功能差异重要的残基,通过重组DNA技术构建了C4A-C4B杂合蛋白。通过溶血试验和与IgG聚集体的结合对这些进行比较表明,1106位的组氨酸被天冬氨酸单取代在很大程度上解释了功能活性的变化以及形成的化学键的性质(酯键与酰胺键)。令人惊讶的是,1106位的组氨酸被中性残基丙氨酸取代导致与免疫聚集体的结合增加,而随后溶血活性并未降低。该结果强烈表明,1106位并非如先前所提出的那样具有“催化性”,而是通过空间/静电与潜在受体位点相互作用,并用于“选择”潜在受体分子上的结合位点。