| p-Benzylthiocarbamoyl-aspartyl-daunorubicin-substituted polytrisacryl. A new drug acid-labile arm-carrier conjugate. | |
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MedLine Citation:
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PMID: 3169016 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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A new type of drug acid-labile arm-carrier is described. A hydrophilic polymer [polytrisacryl, or poly(acryloyl 2-amido-2-hydroxymethyl-1,3-propanediol)], used as a model, is substituted with p-nitrobenzyl groups. The nitrobenzyl groups are reduced to aminobenzyl and transformed into benzylisothiocyanate groups which are allowed to react with aminoacyl daunorubicin. The excess of benzylisothiocyanate is transformed into benzylthiocarbamoyl N-methyl glucamine. A conjugate containing benzylthiocarbamoyl-aspartyl daunorubicin is stable at neutral pH, and releases free daunorubicin when it is exposed to pH 5 or below. This conjugate is about 200-fold less toxic than free daunorubicin, on a molecular basis, when it is added to the medium of Lewis lung carcinoma (3LL) cells in culture. |
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Authors:
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F Daussin; E Boschetti; F Delmotte; M Monsigny |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: European journal of biochemistry / FEBS Volume: 176 ISSN: 0014-2956 ISO Abbreviation: Eur. J. Biochem. Publication Date: 1988 Oct |
Date Detail:
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Created Date: 1988-11-22 Completed Date: 1988-11-22 Revised Date: 2007-07-23 |
Medline Journal Info:
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Nlm Unique ID: 0107600 Medline TA: Eur J Biochem Country: GERMANY, WEST |
Other Details:
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Languages: eng Pagination: 625-8 Citation Subset: IM |
Affiliation:
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Laboratoire de Biochimie Cellulaire et Moléculaire des Glycoconjugués, Centre de Biophysique Moléculaire, Centre National de la Recherche Scientifique, Orléans, France. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Acrylates
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toxicity* Aspartic Acid / toxicity Binding Sites Carcinoma / metabolism Cell Survival / drug effects Daunorubicin / analogs & derivatives*, toxicity Hydrogen-Ion Concentration Lung Neoplasms / metabolism Thiocarbamates / toxicity Tumor Cells, Cultured Vehicles* |
| Chemical | |
Reg. No./Substance:
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0/Acrylates; 0/Thiocarbamates; 0/Vehicles; 20830-81-3/Daunorubicin; 56-84-8/Aspartic Acid; 79-10-7/acrylic acid |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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