Brief Communication HIV-1 rev Antisense Phosphorothioate Oligonucleotide Binding to Human Mononuclear Cells Is Cell Type Specific and Inducible

A fluorescein-conjugated, antisense phosphorothioate oligonucleotide with specificity for HIV-1 rev sequence (FA M-anti-rev) was investigated for its ability to bind to specific subsets of human peripheral blood mononu¬ clear cells. Oligonucleotide binding by CD4+ and CD8+ cells, cells, and monocytes isolated from 15 normal and 15 HIV-infected individuals was evaluated on both nonstimulated mononuclear cells and after 24-hr acti¬ vation with phytohemagglutinin (PHA). In both normals and HI V-infected individuals, we found a signifi¬ cantly higher percentage of monocytes and cells binding oligonucleotide in comparison to cells. Oligonucleotide binding by both cells and cells was enhanced by 24-hr PHA stimulation while monocyte uptake was unchanged. In comparison to normal controls, HIV-1-infected patients showed slightly higher per¬ centages of both unstimulated and PHA activated CD4+, CD8+, and CD25+ cells binding oligonucleotide. The propensity for a high percentage of monocytes, which may act as an HIV-1 reservoir, to bind the anti-rev oligonucleotide and the enhanced binding by cells in the HIV-1-infected patient samples provides some opti¬ mism for potential in vivo therapy of HIV-1 infection using antisense oligonucleotides.