Shibata-Koyama Mami, Iida Shigeru, Okazaki Akira, Mori Katsuhiro, Kitajima-Miyama Kazuko, Saitou Seiji, Kakita Shingo, Kanda Yutaka, Shitara Kenya, Kato Koichi, Satoh Mitsuo
Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd, 3-6-6 Asahi-machi, Machida-shi, Tokyo, Japan.
Glycobiology. 2009 Feb;19(2):126-34. doi: 10.1093/glycob/cwn110. Epub 2008 Oct 24.
Human leukocyte receptor IIIa (Fc gamma RIIIa) plays an important role in mediating therapeutic antibodies' antibody-dependent cellular cytotoxicity (ADCC), which is closely related to the clinical efficacy of anticancer processes in humans in vivo. The removal of the core fucose from oligosaccharides attached to the Fc region of antibodies improves Fc gamma RIIIa binding, allowing the antibodies to enhance dramatically the antibody effector functions of ADCC. In this study, the contribution of Fc gamma RIIIa oligosaccharides to the strength of the Fc gamma RIIIa/antibody complex was analyzed using a serial set of soluble human recombinant Fc gamma RIIIa lacking the oligosaccharides. A nonfucosylated antibody IgG1 appeared to have a significantly higher affinity to the wild-type Fc gamma RIIIa fully glycosylated at its five N-linked oligosaccharide sites than did the fucosylated IgG1, and this increased binding was almost abolished once all of the Fc gamma RIIIa glycosylation was removed. Our gain-of-function analysis in the Fc gamma RIIIa oligosaccharide at Asn-162 (N-162) confirmed that N-162 is the element required for the high binding affinity to nonfucosylated antibodies, as previously revealed by loss-of-function analyses. Interestingly, beyond our expectation, the Fc gamma RIIIa modified by N-162 alone showed a significantly higher binding affinity to nonfucosylated IgG1 than did the wild-type Fc gamma RIIIa. Attachment of the other four oligosaccharides, especially the Fc gamma RIIIa oligosaccharide at Asn-45 (N-45), hindered the high binding affinity of Fc gamma RIIIa to nonfucosylated IgG1. Our data clearly demonstrated that N-45 is an inhibitory element for the high Fc gamma RIIIa binding affinity mediated by N-162 to nonfucosylated antibodies. This information can be exploited for the structural-based functional study of Fc gamma RIIIa.
人白细胞受体IIIa(FcγRIIIa)在介导治疗性抗体的抗体依赖性细胞毒性(ADCC)中起重要作用,这与体内人类抗癌过程的临床疗效密切相关。从连接到抗体Fc区域的寡糖中去除核心岩藻糖可改善FcγRIIIa结合,使抗体能够显著增强ADCC的抗体效应功能。在本研究中,使用一系列缺乏寡糖的可溶性人重组FcγRIIIa分析了FcγRIIIa寡糖对FcγRIIIa/抗体复合物强度的贡献。非岩藻糖基化抗体IgG1对在其五个N-连接寡糖位点完全糖基化的野生型FcγRIIIa的亲和力似乎明显高于岩藻糖基化的IgG1,并且一旦去除所有FcγRIIIa糖基化,这种增加的结合几乎消失。我们对Asn-162(N-162)处的FcγRIIIa寡糖进行的功能获得分析证实,N-162是对非岩藻糖基化抗体具有高结合亲和力所需的元件,如先前功能丧失分析所揭示的那样。有趣的是,出乎我们意料的是,仅由N-162修饰的FcγRIIIa对非岩藻糖基化IgG1的结合亲和力明显高于野生型FcγRIIIa。其他四种寡糖的连接,特别是Asn-45(N-45)处的FcγRIIIa寡糖,阻碍了FcγRIIIa对非岩藻糖基化IgG1的高结合亲和力。我们的数据清楚地表明,N-45是N-162介导的FcγRIIIa对非岩藻糖基化抗体高结合亲和力的抑制元件。该信息可用于基于结构的FcγRIIIa功能研究。