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Delivery of liposomes into cultured KB cells via folate receptor-mediated endocytosis

Folic acid was covalently conjugated to 66-nm liposomes via spacers of various lengths in an attempt to target the liposomes to KB cells expressing folate receptors. Spacers of short and intermediate lengths were unable to mediate association of folate-conjugated liposomes with receptor-bearing cell...

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Published in:The Journal of biological chemistry 1994-02, Vol.269 (5), p.3198-3204
Main Authors: LEE, R. J, LOW, P. S
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Language:English
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cited_by cdi_FETCH-LOGICAL-c438t-ac7f45cc390f97bc0effee13227bbefb703661a08ae0ed26f2e4e8ba664a89fd3
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container_title The Journal of biological chemistry
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description Folic acid was covalently conjugated to 66-nm liposomes via spacers of various lengths in an attempt to target the liposomes to KB cells expressing folate receptors. Spacers of short and intermediate lengths were unable to mediate association of folate-conjugated liposomes with receptor-bearing cells, however, use of a 250 A polyethyleneglycol spacer (PEG, M(r) approximately 3350) permitted avid uptake of the liposomes at approximately 2.5 x 10(5) sites/cell. The binding of folate-PEG liposomes to KB cells could be competitively inhibited by excess free folate or by antiserum against the folate receptor, demonstrating the interaction is mediated by the cell surface folate-binding protein. Following binding, cell-associated folate-PEG liposomes were internalized by folate-receptor-mediated endocytosis at 37 degrees C but not at 4 degrees C. These folate-PEG liposomes show potential for delivering large quantities of low molecular weight compounds nondestructively into folate receptor-bearing cells.
doi_str_mv 10.1016/S0021-9258(17)41848-5
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ispartof The Journal of biological chemistry, 1994-02, Vol.269 (5), p.3198-3204
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subjects Biological and medical sciences
Biological Transport - drug effects
Carrier Proteins - metabolism
Diverse techniques
Drug Carriers
Endocytosis - drug effects
Folate Receptors, GPI-Anchored
Folic Acid - analogs & derivatives
Folic Acid - pharmacology
Fundamental and applied biological sciences. Psychology
Humans
Immune Sera - pharmacology
KB Cells
Kinetics
Liposomes
Molecular and cellular biology
Polyethylene Glycols
Receptors, Cell Surface
title Delivery of liposomes into cultured KB cells via folate receptor-mediated endocytosis
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