Abstract
Advances in the molecular biology of oncogenesis have established a key role for transcription factors in malignant transformation. In some cases the activity of the transcription factor itself is altered by mutation. In many other cases, the activity of the transcription factor is affected by mutations in upstream signaling or regulatory proteins. This review highlights four transcription factors - Stat3, Stat5, NF-kB, and HIF-1 - which are associated with cancer development. The evidence for the involvement of these factors in oncogenesis is reviewed. Further, we examine the efforts to specifically target these transcription factors for therapeutic intervention. Such strategies include using peptidomimetics, antisense oligonucleotides, small molecule inhibitors, and G-quartet oligonucleotides. Inhibition of transcription factor activity may occur at the level of activation, translocation, or DNA binding. Application of these approaches to in vitro and in vivo models of tumorigenesis is discussed.
Keywords: ap family, apoptosis, oncogenesis, stats, src-homology (sh), janus kinases (jaks), reporter gene assays, oligodeoxynucleotides
Current Pharmaceutical Design
Title: Targeting Transcription Factors for Cancer Therapy
Volume: 11 Issue: 22
Author(s): M. S. Redell and D. J. Tweardy
Affiliation:
Keywords: ap family, apoptosis, oncogenesis, stats, src-homology (sh), janus kinases (jaks), reporter gene assays, oligodeoxynucleotides
Abstract: Advances in the molecular biology of oncogenesis have established a key role for transcription factors in malignant transformation. In some cases the activity of the transcription factor itself is altered by mutation. In many other cases, the activity of the transcription factor is affected by mutations in upstream signaling or regulatory proteins. This review highlights four transcription factors - Stat3, Stat5, NF-kB, and HIF-1 - which are associated with cancer development. The evidence for the involvement of these factors in oncogenesis is reviewed. Further, we examine the efforts to specifically target these transcription factors for therapeutic intervention. Such strategies include using peptidomimetics, antisense oligonucleotides, small molecule inhibitors, and G-quartet oligonucleotides. Inhibition of transcription factor activity may occur at the level of activation, translocation, or DNA binding. Application of these approaches to in vitro and in vivo models of tumorigenesis is discussed.
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Cite this article as:
Redell S. M. and Tweardy J. D., Targeting Transcription Factors for Cancer Therapy, Current Pharmaceutical Design 2005; 11 (22) . https://dx.doi.org/10.2174/1381612054546699
DOI https://dx.doi.org/10.2174/1381612054546699 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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