Synthesis of an immunoconjugate of camptothecin

被引：36

作者：

Walker, MA ^{[1
]}

Dubowchik, GM ^{[1
]}

Hofstead, SJ ^{[1
]}

Trail, PA ^{[1
]}

Firestone, RA ^{[1
]}

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Wallingford, CT 06492 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(01)00707-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The first immunoconjugate of camptothecin has been synthesized wherein the drug is attached to the tumor-recognizing antibody BR96 via a Cathepsin B cleavable linker. Endocytosis of the immunoconjugate upon binding to the tumor cell followed by enzymatic cleavage of the linker inside the endosome ensures tumor-specific release of the drug. In this way, it is hoped that the dose-limiting side effects associated with camptothecin can be eliminated while the antitumor activity is preserved. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：217 / 219

页数：3

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