Multiple catalytic aldolase antibodies suitable for chemical programming

Multiple catalytic aldolase antibodies suitable for chemical programming
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DOI:
10.1016/j.bmcl.2009.04.041
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发表时间:
2009-07-15
影响因子:
2.7
通讯作者:
Sinha, Subhash C.
Sinha, Subhash C.
中科院分区:
医学4区
文献类型:
--
作者:
Goswami, Rajib Kumar;Huang, Zheng-Zheng;Sinha, Subhash C.

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使用配备有抑制整联蛋白粘附受体功能的二酮或前乙烯基酮接头的化合物检查具有催化醛缩酶活性的九种鼠抗体的化学编程。结果显示,大多数抗体以与先前报道的催化抗体38C2类似的方式使用二酮化合物编程。另一方面,仅对有效催化原乙烯基酮接头的逆向羟醛缩合反应的那些抗体进行编程。与整联蛋白靶向化合物偶联,至少三种新抗体,包括84 G3、85 H6和90 G8,表现出与表达整联蛋白α v β的人肿瘤细胞的高度特异性结合(3)。(C)2009爱思唯尔有限公司版权所有。
Chemical programming of nine murine antibodies with catalytic aldolase activity was examined using compounds, equipped with diketone or pro-vinyl ketone linkers that inhibit integrin adhesion receptor functions. The results showed that most Abs were programmed using the diketone compounds in a manner similar to previously reported catalytic antibody 38C2. On the other hand, only those antibodies, which catalyzed the retro aldol reaction of the pro-vinyl ketone linkers efficiently, were programmed. Conjugated to integrin targeting compounds, at least three new antibodies, including 84G3, 85H6, and 90G8, exhibited high specific binding to human tumor cells expressing integrin alpha v beta(3). (C) 2009 Elsevier Ltd. All rights reserved.