Document 0021 DOCN M9580021 TI Gene-targeted inhibition of transactivation of human immunodeficiency virus type-1 (HIV-1)-LTR by antisense oligonucleotides. DT 9506 AU Demirhan I; Hasselmayer O; Hofmann D; Chandra A; Svinarchuk FP; Vlassov VV; Engels J; Chandra P; Laboratory of Molecular Biology, Frankfurt University School of; Medicine, FRG. SO Virus Genes. 1995 Jan;9(2):113-9. Unique Identifier : AIDSLINE MED/95250303 AB We have used an in vitro approach to study the efficiency of antisense oligonucleotides in inhibiting LTR-(HIV-1)-directed CAT expression catalyzed by tat protein, the functional protein of the transactivator gene. We selected the target sequence localized near the 5' end of the tat mRNA. The following conclusions can be drawn from the data presented here: a) Antisense oligonucleotides modified by conjugation of cholesterol at the 3' end have a severalfold higher inhibitory response, b) inhibitory response is dependent on the mode of introducing oligonucleotides, and c) the inhibition by antisense oligonucleotides is sequence specific and directed towards the targeted region. This approach could be useful for targeting functional regions of regulatory gene products and designing gene-targeted inhibitors of virus replication. DE Animal Base Sequence Cats/GENETICS Cell Line Gene Products, tat/GENETICS/METABOLISM *Gene Targeting Human HIV Long Terminal Repeat/*GENETICS HIV-1/GENETICS Molecular Sequence Data Oligonucleotides, Antisense/*PHARMACOLOGY Trans-Activation (Genetics)/*DRUG EFFECTS JOURNAL ARTICLE SOURCE: National Library of Medicine. NOTICE: This material may be protected by Copyright Law (Title 17, U.S.Code).