Molecular targeting of nuclear transcriptional regulators.
Rojanasakul-Y; Luo-Q; Ye-J; Faroonsargn-D; Dokka-S; Shi-X
Controlled Drug Delivery: Designing Technologies for the Future. American Chemical Society (ACS) Symposium Series 752. Park K, Mrsny RJ, eds., Washington, DC: American Chemical Society, 2000 May; :193-200
Gene regulation by nuclear transcription factors involves intracellular interactions of nuclear transcriptors with specific transport carriers and/or DNA regulatory elements using sequence-specific recognition sites. In this study, we utilized a series of synthetic peptides carrying the nuclear localization sequence of the transcriptor NF-KB p50 and p65 subunits to inhibit NF-KB-mediated gene expression. Gene transfection and gel-shift assays showed that these peptides were effective in inhibiting the nuclear translocation and transcriptional activation of NF-KB. However, their effects required the presence of a cell-permeable peptide which is covalently linked to the inhibitory peptides. These hybrid peptides may be used as novel therapeutic agents in diseases whose etiology is dependent on NF-KB activation.
Genetics; Genes; Treatment; Therapeutic-agents
Book or book chapter
Controlled Drug Delivery: Designing Technologies for the Future. American Chemical Society (ACS) Symposium Series 752