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

Authors
Mandler, R Dadachova, E Brechbiel, JK Waldmann, TA Brechbiel, MW
Citation
R. Mandler et al., Synthesis and evaluation of antiproliferative activity of a geldanamycin-Herceptin (TM) immunoconjugate, BIOORG MED, 10(10), 2000, pp. 1025-1028
Citations number
27
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
10
Year of publication
2000
Pages
1025 - 1028
Database
ISI
SICI code
0960-894X(20000515)10:10<1025:SAEOAA>2.0.ZU;2-D
Abstract
Geldanamycin was modified with 1,4-diaminobutane to introduce a primary ami ne that was subsequently employed to provide a maleimide for protein linkag e. Monoclonal antibody Herceptin(TM) was then derivatized to generate thiol groups that reacted with the maleimide derivative to produce the immunocon jugate. The product showed antiproliferative activity greater than native H erceptin(TM). (C) 2000 Elsevier Science Ltd. All rights reserved.