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

Raya Mandler, Ekaterina Dadachova, James K. Brechbiel, Thomas A. Waldmann, Martin W. Brechbiel

Research output: Contribution to journalArticle

13 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)1025-1028
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume10
Issue number10
DOIs
StatePublished - May 15 2000

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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