Synthesis and evaluation of antiproliferative activity of a geldanamycin-Herceptin™ immunoconjugate

被引：14

作者：

Mandler, R

Dadachova, E

Brechbiel, JK

Waldmann, TA

Brechbiel, MW ^{[1
]}

机构：

[1] NCI, Radioimmune & Inorgan Chem Sect, Radiat Oncol Branch, NIH, Bethesda, MD 20982 USA

[2] NCI, Metab Branch, NIH, Bethesda, MD 20982 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(00)00155-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Geldanamycin was modified with 1,4-diaminobutane to introduce a primary amine that was subsequently employed to provide a maleimide for protein linkage. Monoclonal antibody Herceptin(TM) was then derivatized to generate thiol groups that reacted with the maleimide derivative to produce the immunoconjugate. The product showed antiproliferative activity greater than native Herceptin(TM). (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：1025 / 1028

页数：4

共 29 条

[1] Phase II study of weekly intravenous recombinant humanized Anti-p185(HER2) monoclonal antibody in patients with HER2/neu-overexpressing metastatic breast [J].