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

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

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 journal › Article › peer-review

17 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 language	English (US)
Pages (from-to)	1025-1028
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	10
Issue number	10
DOIs	https://doi.org/10.1016/S0960-894X(00)00155-4
State	Published - May 15 2000
Externally published	Yes

ASJC Scopus subject areas

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

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

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AU - Mandler, Raya

AU - Dadachova, Ekaterina

AU - Brechbiel, James K.

AU - Waldmann, Thomas A.

AU - Brechbiel, Martin W.

PY - 2000/5/15

Y1 - 2000/5/15

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

Abstract

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