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 Citations (Scopus)

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
Externally publishedYes

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Immunoconjugates
Putrescine
Sulfhydryl Compounds
Amines
Monoclonal Antibodies
Derivatives
Proteins
Trastuzumab
geldanamycin
maleimide

ASJC Scopus subject areas

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

Cite this

Synthesis and evaluation of antiproliferative activity of a geldanamycin-Herceptin(TM) immunoconjugate. / Mandler, Raya; Dadachova, Ekaterina; Brechbiel, James K.; Waldmann, Thomas A.; Brechbiel, Martin W.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 10, No. 10, 15.05.2000, p. 1025-1028.

Research output: Contribution to journalArticle

Mandler, Raya ; Dadachova, Ekaterina ; Brechbiel, James K. ; Waldmann, Thomas A. ; Brechbiel, Martin W. / Synthesis and evaluation of antiproliferative activity of a geldanamycin-Herceptin(TM) immunoconjugate. In: Bioorganic and Medicinal Chemistry Letters. 2000 ; Vol. 10, No. 10. pp. 1025-1028.
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