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M9640545.TXT
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1996-03-04
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Document 0545
DOCN M9640545
TI Endosomolytic activity of cationic liposomes enhances the delivery of
human immunodeficiency virus-1 trans-activator protein (TAT) to
mammalian cells.
DT 9604
AU Huang L; Farhood H; Serbina N; Teepe AG; Barsoum J; Department of
Pharmacology, University of Pittsburgh, School of; Medicine, PA 15261,
USA.
SO Biochem Biophys Res Commun. 1995 Dec 26;217(3):761-8. Unique Identifier
: AIDSLINE MED/96125309
AB We have explored the use of cationic liposomes to deliver the human
immunodeficiency virus-1 trans-activator protein tat using a reporter
gene expression assay. The human epidermoid carcinoma cell A431 stably
transfected with a reporter gene under the control of human
immunodeficiency virus-1 promoter was used as a target cell.
Phosphatidylcholine-containing cationic liposomes had no detectable tat
delivery activity. In contrast, delivery of tat was enhanced by up to
150-fold using cationic liposomes enriched with dioleoyl
phosphatidylethanolamine (DOPE), a lipid which readily transforms a
bilayer into a nonbilayer structure. Enhanced delivery of tat by
DOPE-containing liposomes was most likely the result of the
endosomolytic activity of the liposome. This phospholipid-rich
formulation showed no toxicity at concentrations sufficient for maximal
delivery of tat. A variety of cationic liposome formulations which
contain DOPE were tested successfully for tat delivery.
DE Cations Drug Delivery Systems Endocytosis Endosomes/CHEMISTRY Gene
Products, tat/*ADMINISTRATION & DOSAGE Human HIV-1
Liposomes/*CHEMISTRY Support, U.S. Gov't, P.H.S. Tumor Cells, Cultured
JOURNAL ARTICLE
SOURCE: National Library of Medicine. NOTICE: This material may be
protected by Copyright Law (Title 17, U.S.Code).