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Targeting of neoglycoprotein-drug conjugates to cultured human embryonal carcinoma cells

Standard

Targeting of neoglycoprotein-drug conjugates to cultured human embryonal carcinoma cells. / Gabius, H J; Bokemeyer, C; Hellmann, T; Schmoll, H J.

in: J CANCER RES CLIN, Jahrgang 113, Nr. 2, 1987, S. 126-30.

Publikationen: SCORING: Beitrag in Fachzeitschrift/Zeitung › SCORING: Zeitschriftenaufsatz › Forschung › Begutachtung

Harvard

Gabius, HJ, Bokemeyer, C, Hellmann, T & Schmoll, HJ 1987, 'Targeting of neoglycoprotein-drug conjugates to cultured human embryonal carcinoma cells', J CANCER RES CLIN, Jg. 113, Nr. 2, S. 126-30.

APA

Gabius, H. J., Bokemeyer, C., Hellmann, T., & Schmoll, H. J. (1987). Targeting of neoglycoprotein-drug conjugates to cultured human embryonal carcinoma cells. J CANCER RES CLIN, 113(2), 126-30.

Vancouver

Gabius HJ, Bokemeyer C, Hellmann T, Schmoll HJ. Targeting of neoglycoprotein-drug conjugates to cultured human embryonal carcinoma cells. J CANCER RES CLIN. 1987;113(2):126-30.

Bibtex

@article{695b8c06ea5c412e8ed6f9bc9bb306bf,
title = "Targeting of neoglycoprotein-drug conjugates to cultured human embryonal carcinoma cells",
abstract = "Fluorescent neoglycoproteins were used to screen for the presence and sugar specificities of cell surface lectins in two human embryonal carcinoma cell lines. Efficient labeling correlated with extent of lectin-mediated uptake of neoglycoproteins, as measured by inhibition of DNA synthesis by drug-neoglycoprotein conjugates. These conjugates contain covalently linked carbohydrate moieties on the carriers to render them accessible to the membrane lectins, most effectively galactosides and alpha-glucosides. They furthermore contain chemically linked cytotoxic drugs (etoposide, cis-diamminedichloroplatinum II and methotrexate) which are intracellularly released after lysosomal breakdown of the carrier, as indicated by the effect of leupeptin. Sugars can confer a greater than 10-fold increase in cytotoxic capacity to the nonglycosylated carrier-drug conjugate, nearly reaching the level of toxicity of the freely diffusible drug. Two different neoglycoproteins, reacting with independently targeted membrane lectins, were shown to be useful in a model for combination chemotherapy. These results therefore suggest potential usefulness of custom-made glycosylated carriers in the targeting of therapeutic agents to human embryonal carcinoma cells.",
keywords = "Antineoplastic Agents, Cell Line, Cell Survival, Cisplatin, Etoposide, Glycoproteins, Humans, Lectins, Leupeptins, Methotrexate, Pharmaceutical Vehicles, Receptors, Cell Surface, Teratoma",
author = "Gabius, {H J} and C Bokemeyer and T Hellmann and Schmoll, {H J}",
year = "1987",
language = "English",
volume = "113",
pages = "126--30",
journal = "J CANCER RES CLIN",
issn = "0171-5216",
publisher = "Springer",
number = "2",

}

RIS

TY - JOUR

T1 - Targeting of neoglycoprotein-drug conjugates to cultured human embryonal carcinoma cells

AU - Gabius, H J

AU - Bokemeyer, C

AU - Hellmann, T

AU - Schmoll, H J

PY - 1987

Y1 - 1987

N2 - Fluorescent neoglycoproteins were used to screen for the presence and sugar specificities of cell surface lectins in two human embryonal carcinoma cell lines. Efficient labeling correlated with extent of lectin-mediated uptake of neoglycoproteins, as measured by inhibition of DNA synthesis by drug-neoglycoprotein conjugates. These conjugates contain covalently linked carbohydrate moieties on the carriers to render them accessible to the membrane lectins, most effectively galactosides and alpha-glucosides. They furthermore contain chemically linked cytotoxic drugs (etoposide, cis-diamminedichloroplatinum II and methotrexate) which are intracellularly released after lysosomal breakdown of the carrier, as indicated by the effect of leupeptin. Sugars can confer a greater than 10-fold increase in cytotoxic capacity to the nonglycosylated carrier-drug conjugate, nearly reaching the level of toxicity of the freely diffusible drug. Two different neoglycoproteins, reacting with independently targeted membrane lectins, were shown to be useful in a model for combination chemotherapy. These results therefore suggest potential usefulness of custom-made glycosylated carriers in the targeting of therapeutic agents to human embryonal carcinoma cells.

AB - Fluorescent neoglycoproteins were used to screen for the presence and sugar specificities of cell surface lectins in two human embryonal carcinoma cell lines. Efficient labeling correlated with extent of lectin-mediated uptake of neoglycoproteins, as measured by inhibition of DNA synthesis by drug-neoglycoprotein conjugates. These conjugates contain covalently linked carbohydrate moieties on the carriers to render them accessible to the membrane lectins, most effectively galactosides and alpha-glucosides. They furthermore contain chemically linked cytotoxic drugs (etoposide, cis-diamminedichloroplatinum II and methotrexate) which are intracellularly released after lysosomal breakdown of the carrier, as indicated by the effect of leupeptin. Sugars can confer a greater than 10-fold increase in cytotoxic capacity to the nonglycosylated carrier-drug conjugate, nearly reaching the level of toxicity of the freely diffusible drug. Two different neoglycoproteins, reacting with independently targeted membrane lectins, were shown to be useful in a model for combination chemotherapy. These results therefore suggest potential usefulness of custom-made glycosylated carriers in the targeting of therapeutic agents to human embryonal carcinoma cells.

KW - Antineoplastic Agents

KW - Cell Line

KW - Cell Survival

KW - Cisplatin

KW - Etoposide

KW - Glycoproteins

KW - Humans

KW - Lectins

KW - Leupeptins

KW - Methotrexate

KW - Pharmaceutical Vehicles

KW - Receptors, Cell Surface

KW - Teratoma

M3 - SCORING: Journal article

C2 - 3031079

VL - 113

SP - 126

EP - 130

JO - J CANCER RES CLIN

JF - J CANCER RES CLIN

SN - 0171-5216

IS - 2

ER -