TY - JOUR
T1 - The synthesis and characterization of polypeptide-adriamycin conjugates and its complexes with adriamycin
T2 - Part I
AU - Heeswijk, W.A.R.
AU - Hoes, C.J.T.
AU - Stoffer, T.
AU - Eenink, M.J.D.
AU - Potman, W.
AU - Feijen, J.
PY - 1985
Y1 - 1985
N2 - 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.
AB - 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.
U2 - 10.1016/0168-3659(85)90006-9
DO - 10.1016/0168-3659(85)90006-9
M3 - Article
VL - 1
SP - 301
EP - 315
JO - Journal of controlled release
JF - Journal of controlled release
SN - 0168-3659
IS - 4
ER -