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.
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Authors | A Ahmad, K L Law, B Young, M W Telander, J R Ogden, K Leung |
Journal | Anticancer research
(Anticancer Res)
1990 May-Jun
Vol. 10
Issue 3
Pg. 837-43
ISSN: 0250-7005 [Print] Greece |
PMID | 2369097
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Antibodies, Monoclonal
- Indicators and Reagents
- aconitic anhydride
- Aconitic Acid
- Daunorubicin
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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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