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

Autor: M.J.D. Eenink, W. Potman, W.A.R. Heeswijk, T. Stoffer, Jan Feijen, C.J.T. Hoes
Přispěvatelé: Faculty of Science and Technology, Biomaterials Science and Technology
Jazyk: angličtina
Rok vydání: 1985
Předmět:
Zdroj: Journal of controlled release, 1(4), 301-315. Elsevier
ISSN: 0168-3659
DOI: 10.1016/0168-3659(85)90006-9
Popis: 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.
Databáze: OpenAIRE