ArticleNucleic acids research2003
Selective inhibition of transcription of the Ets2 gene in prostate cancer cells by a triplex-forming oligonucleotide.
Article in Nucleic acids research, 2003. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 55 citations in OpenAlex.
- Targeted DNA triplex-forming oligonucleotide liposome for pulmonary fibrosis gene therapy.Cell reports. Medicine · 2026Article
- A compendium of Androgen Receptor Variant 7 target genes and their role in Castration Resistant Prostate Cancer.Frontiers in oncology · 2023Review
- Triplex-forming oligonucleotides as an anti-gene technique for cancer therapy.Frontiers in pharmacology · 2022Review
- LncRNA MIR100HG promotes cell proliferation in triple-negative breast cancer through triplex formation with p27 loci.Cell death & disease · 2018Article
- Interaction of 9-O-(ω-amino) alkyl ether berberine analogs with poly(dT)·poly(dA)*poly(dT) triplex and poly(dA)·poly(dT) duplex: a comparative study.Molecular biology reports · 2013Article
- Understanding the role of ETS-mediated gene regulation in complex biological processes.Advances in cancer research · 2013Review
- Regulation of transcription through light-activation and light-deactivation of triplex-forming oligonucleotides in mammalian cells.ACS chemical biology · 2012Article
- Selection of RNA aptamers that bind HIV-1 LTR DNA duplexes: strand invaders.Nucleic acids research · 2010Article
- Article
- Calorimetric and spectroscopic studies of aminoglycoside binding to AT-rich DNA triple helices.Biochimie · 2010Article
- The triple helix: 50 years later, the outcome.Nucleic acids research · 2008Review
- Review
- Purine twisted-intercalating nucleic acids: a new class of anti-gene molecules resistant to potassium-induced aggregation.Nucleic acids research · 2008Article
- Novel GC-rich DNA-binding compound produced by a genetically engineered mutant of the mithramycin producer Streptomyces argillaceus exhibits improved transcriptional repressor activity: implications for cancer therapy.Nucleic acids research · 2006Article
- New insights into DNA triplexes: residual twist and radial difference as measures of base triplet non-isomorphism and their implication to sequence-dependent non-uniform DNA triplex.Nucleic acids research · 2005Article
- Triplex DNA-mediated downregulation of Ets2 expression results in growth inhibition and apoptosis in human prostate cancer cells.Nucleic acids research · 2004Article
- DNA binding and antigene activity of a daunomycin-conjugated triplex-forming oligonucleotide targeting the P2 promoter of the human c-myc gene.Nucleic acids research · 2004Article
- Therapeutic modulation of endogenous gene function by agents with designed DNA-sequence specificities.Nucleic acids research · 2003Review
- Effect of DNA target sequence on triplex formation by oligo-2'-deoxy- and 2'-O-methylribonucleotides.Nucleic acids research · 2003Article
- Review
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
The transcription factor Ets2 has a role in cancer development and represents an attractive therapeutic target. In this study, we designed a triplex-forming oligonucleotide (TFO) directed to a homopurine:homopyrimidine sequence in the Ets2 promoter. Transcription factors of the Sp family bound to this sequence and mutation of the Sp1 site reduced Ets2 promoter activity. The Ets2-TFO had high binding affinity for the target sequence and inhibited binding of Sp1/Sp3 to the overlapping site. This effect occurred with a high degree of sequence specificity. Mismatched oligonucleotides did not inhibit Sp1/Sp3 binding and mutations in the target sequence that abolished triplex formation prevented inhibition of Sp1/Sp3 binding by the TFO. The Ets2-TFO inhibited Ets2 promoter activity and expression of the endogenous gene in prostate cancer cells at nanomolar concentrations. The TFO did not affect reporter constructs with mutations in the TFO binding site and promoters of non-targeted genes. Expression of non-targeted genes was also not affected in TFO-treated cells. Collectively, these data demonstrated that the anti-transcriptional activity of the Ets2-TFO was sequence- and target-specific, and ruled out alternative, non-triplex mediated mechanisms of action. This anti-transcriptional approach may be useful to examine the effects of selective downregulation of Ets2 expression and may have therapeutic applications.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.