Chemically programmed antibodies:: Endothelin receptor targeting CovX-Bodies™

被引：45

作者：

Doppalapudi, Venkata R. ^{[1
]}

Tryder, Nancy ^{[1
]}

Li, Lingna ^{[1
]}

Aja, Teresa ^{[1
]}

Griffith, David ^{[1
]}

Liao, Francesca-Fang ^{[1
]}

Roxas, Giovanni ^{[1
]}

Ramprasad, Mysore P. ^{[1
]}

Bradshaw, Curt ^{[1
]}

Barbas, Carlos F., III ^{[1
]}

机构：

[1] CovX Res LLC, San Diego, CA 92130 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 02期

关键词：

monoclonal antibodies; aldolase antibody; CovX-Body (TM); endothelin-A; endothelin-A (ETA) antagonists; antitumor efficacy;

D O I：

10.1016/j.bmcl.2006.10.009

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

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页码：501 / 506

页数：6

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