人CD20单克隆抗体的生物学活性与CD20上独特的表位相关。

The biological activity of human CD20 monoclonal antibodies is linked to unique epitopes on CD20.

作者信息

Teeling Jessica L, Mackus Wendy J M, Wiegman Luus J J M, van den Brakel Jeroen H N, Beers Stephen A, French Ruth R, van Meerten Tom, Ebeling Saskia, Vink Tom, Slootstra Jerry W, Parren Paul W H I, Glennie Martin J, van de Winkel Jan G J

机构信息

Genmab, Utrecht, The Netherlands.

出版信息

J Immunol. 2006 Jul 1;177(1):362-71. doi: 10.4049/jimmunol.177.1.362.

Abstract

We have previously defined a panel of fully human CD20 mAb. Most of these were unexpectedly efficient in their ability to recruit C1q to the surface of CD20-positive cells and mediate tumor lysis via activation of the classical pathway of complement. This complement-dependent cytotoxicity (CDC) potency appeared to relate to the unusually slow off-rate of these human Abs. However, we now present epitope-mapping data, which indicates that all human mAb bind a novel region of CD20 that may influence CDC potency. Epitope mapping, using both mutagenesis studies and overlapping 15-mer peptides of the extracellular loops of CD20, defined the amino acids required for binding by an extensive panel of mouse and human mAb. Binding by rituximab and mouse CD20 mAb, had an absolute requirement for alanine and proline at positions 170 and 172, respectively, within the large extracellular loop of CD20. Surprisingly, however, all of the human CD20 mAb recognize a completely novel epitope located N-terminally of this motif, also including the small extracellular loop of CD20. Thus, although off-rate may influence biological activity of mAb, another critical factor for determining CDC potency by CD20 mAb appears to be the region of the target molecule they recognize. We conclude that recognition of the novel epitope cooperates with slow off-rate in determining the activity of CD20 Ab in activation of complement and induction of tumor cell lysis.

摘要

我们之前定义了一组全人源CD20单克隆抗体。其中大多数在将C1q募集到CD20阳性细胞表面并通过激活补体经典途径介导肿瘤细胞裂解方面具有出人意料的高效性。这种补体依赖性细胞毒性(CDC)效力似乎与这些人源抗体异常缓慢的解离速率有关。然而,我们现在展示的表位映射数据表明,所有的人源单克隆抗体都结合CD20的一个新区域,该区域可能影响CDC效力。通过诱变研究和使用CD20细胞外环的重叠15肽进行表位映射,确定了大量小鼠和人源单克隆抗体结合所需的氨基酸。利妥昔单抗和小鼠CD20单克隆抗体的结合,分别对CD20大细胞外环中第170位和第172位的丙氨酸和脯氨酸有绝对需求。然而,令人惊讶的是,所有的人源CD20单克隆抗体都识别位于该基序N端的一个全新表位,该表位还包括CD20的小细胞外环。因此,虽然解离速率可能影响单克隆抗体的生物学活性,但决定CD20单克隆抗体CDC效力的另一个关键因素似乎是它们识别的靶分子区域。我们得出结论,在补体激活和肿瘤细胞裂解诱导中,对新表位的识别与缓慢的解离速率共同作用,决定CD20抗体的活性。

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