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Daunorubicin coupled to monoclonal antibodies via a cis-aconitic anhydride linker: biochemical and cytotoxic properties revisited.

Abstract
Daunorubicin (DNR) was coupled to monoclonal antibodies (Mab) reactive to breast tumor cells using the acid-labile linking agents cis-asonitic anhydride and two other non acid-labile analogs, glutaric anhydride and citraconic anhydride. The acid derivatives of DNR formed by reaction with the anhydrides were converted to their N-hydroxysuccinimide (NHS) active esters for coupling to MAb. The molar input of drug NHS ester to MAb ranged from 1:1 to 100:1. The resulting MAb-DNR conjugates were purified by gel filtration and analyzed by high performance liquid chromatography. Monomeric conjugates contained 0.2 to 11.0 moles of DNR/mole of MAb. No evidence of cell killing was observed up to a concentration of 10 micrograms/ml DNR bound to MAb, while DNR exhibited 50% killing of the breast tumor cell line MCF-7 at a concentration of 1 microgram/ml.
AuthorsA Ahmad, K L Law, B Young, M W Telander, J R Ogden, K Leung
JournalAnticancer research (Anticancer Res) 1990 May-Jun Vol. 10 Issue 3 Pg. 837-43 ISSN: 0250-7005 [Print] Greece
PMID2369097 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antibodies, Monoclonal
  • Indicators and Reagents
  • aconitic anhydride
  • Aconitic Acid
  • Daunorubicin
Topics
  • Aconitic Acid (analogs & derivatives)
  • Antibodies, Monoclonal (isolation & purification, pharmacology)
  • Breast Neoplasms
  • Cell Survival (drug effects)
  • Chromatography, High Pressure Liquid
  • Daunorubicin (pharmacology)
  • Humans
  • Indicators and Reagents
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive
  • Molecular Structure
  • Tumor Cells, Cultured (cytology, drug effects)

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