The synthesis and characterization of polypeptide-adriamycin conjugates and its complexes with adriamycin. Part I

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Heeswijk, W.A.R. and Hoes, C.J.T. and Stoffer, T. and Eenink, M.J.D. and Potman, W. and Feijen, J. (1985) The synthesis and characterization of polypeptide-adriamycin conjugates and its complexes with adriamycin. Part I. Journal of Controlled Release, 1 (4). pp. 301-315. ISSN 0168-3659

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Abstract:Poly(α-l-glutamic acid) (PGA) was grafted with amino acid and oligopeptide spacers up to 5 amino acids with the use of N,N'-carbonyldiimidazole and 2,3-dihydro-1,2-benz-isothiazole-3-on-1, 1-dioxide (saccharin) as an additive, and these polypeptides were characterized. The antitumor antibiotic adriamycin was covalently coupled via an amide bond onto PGA and onto the grafted polymers with the use of N-ethoxycarbonyl-2-ethoxy-1, 2-dihydroquinoline (EEDQ); these conjugates were characterized. The conjugates containing Gly—Gly—l-Leu spacer arms did yield free adriamycin upon digestion with papain. Adriamycin gave fairly stable complexes with PGA—adriamycin and branched poly peptide—adriamycin conjugates; these complexes were characterized.
Item Type:Article
Copyright:© 1985 Elsevier Science
Faculty:
Science and Technology (TNW)
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Link to this item:http://purl.utwente.nl/publications/69411
Official URL:http://dx.doi.org/10.1016/0168-3659(85)90006-9
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