Chemically programmed antibodies:: Endothelin receptor targeting CovX-Bodies™
Chemically programmed antibodies:: Endothelin receptor targeting CovX-Bodies™
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DOI：
10.1016/j.bmcl.2006.10.009
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发表时间：
2007-01-15
影响因子：
2.7
通讯作者：
Barbas, Carlos F., III
中科院分区：
文献类型：
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作者：
Doppalapudi, Venkata R.;Tryder, Nancy;Barbas, Carlos F., III
合成基于芳基磺酰胺的内皮素拮抗剂并将其共价连接至m38C2抗体的反应性赖氨酸以产生一系列CovX体。这些化学程序化抗体在体外表现为有效的内皮素受体拮抗剂，并且在前列腺癌异种移植模型中具有抗肿瘤功效，其在摩尔基础上远远超过母体小分子的活性。(c)2006爱思唯尔有限公司保留所有权利。
Aryl sulfonamide-based endothelin antagonists were synthesized and covalently linked to the reactive lysine of the m38C2 antibody to create a series of CovX-Bodies. These chemically programmed antibodies behaved as potent endothelin receptor antagonists in vitro and had antitumor efficacy in a prostate cancer xenograft model which, on a molar basis, far exceeded the activity of the parent small molecule. (c) 2006 Elsevier Ltd. All rights reserved.