ArticleJournal of the American Chemical Society2009
Cyclic pyrrole-imidazole polyamides targeted to the androgen response element.
Article in Journal of the American Chemical Society, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
29 citing papers in PubMed, 76 citations in OpenAlex.
- Long-Range Allosteric Modulation of DNA Duplex Dynamics Induced by Pyrrole-Imidazole Polyamide Binding.The journal of physical chemistry letters · 2025Article
- Sequence-Selective Recognition of the d(GGCGCC)ACS omega · 2024Article
- Strong and Specific Recognition of CAG/CTG Repeat DNA (5'-dWGCWGCW-3') by a Cyclic Pyrrole-Imidazole Polyamide.Chembiochem : a European journal of chemical biology · 2022Article
- New Opportunities for Targeting the Androgen Receptor in Prostate Cancer.Cold Spring Harbor perspectives in medicine · 2018Review
- Interactions of two large antiviral polyamides with the long control region of HPV16.Biochimie · 2016Article
- Catch and Release DNA Decoys: Capture and Photochemical Dissociation of NF-κB Transcription Factors.ACS chemical biology · 2016Article
- Solution formulation development and efficacy of MJC13 in a preclinical model of castration-resistant prostate cancer.Pharmaceutical development and technology · 2016Article
- Androgen receptor: structure, role in prostate cancer and drug discovery.Acta pharmacologica Sinica · 2015Review
- Article
- Replication stress by Py-Im polyamides induces a non-canonical ATR-dependent checkpoint response.Nucleic acids research · 2014Article
- Article
- Structure-dependent inhibition of the ETS-family transcription factor PU.1 by novel heterocyclic diamidines.Nucleic acids research · 2014Article
- Animal toxicity of hairpin pyrrole-imidazole polyamides varies with the turn unit.Journal of medicinal chemistry · 2013Article
- Synthesis of cyclic Py-Im polyamide libraries.The Journal of organic chemistry · 2013Article
- Pyrrole-imidazole polyamides distinguish between double-helical DNA and RNA.Angewandte Chemie (International ed. in English) · 2013Article
- Binding of hairpin pyrrole and imidazole polyamides to DNA: relationship between torsion angle and association rate constants.Nucleic acids research · 2012Article
- Guiding the design of synthetic DNA-binding molecules with massively parallel sequencing.Journal of the American Chemical Society · 2012Article
- Single-dose pharmacokinetic and toxicity analysis of pyrrole-imidazole polyamides in mice.Cancer chemotherapy and pharmacology · 2012Article
- Characterization and solubilization of pyrrole-imidazole polyamide aggregates.Journal of medicinal chemistry · 2012Article
- Microwave assisted synthesis of Py-Im polyamides.Organic letters · 2012Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Hairpin pyrrole-imidazole (Py-Im) polyamides are a class of cell-permeable DNA-binding small molecules that can disrupt transcription factor-DNA binding and regulate endogenous gene expression. The covalent linkage of antiparallel Py-Im ring pairs with an gamma-amino acid turn unit affords the classical hairpin Py-Im polyamide structure. Closing the hairpin with a second turn unit yields a cyclic polyamide, a lesser-studied architecture mainly attributable to synthetic inaccessibility. We have applied our methodology for solution-phase polyamide synthesis to cyclic polyamides with an improved high-yield cyclization step. Cyclic 8-ring Py-Im polyamides 1-3 target the DNA sequence 5'-WGWWCW-3', which corresponds to the androgen response element (ARE) bound by the androgen receptor transcription factor to modulate gene expression. We find that cyclic Py-Im polyamides 1-3 bind DNA with exceptionally high affinities and regulate the expression of AR target genes in cell culture studies, from which we infer that the cycle is cell permeable.
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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.