ArticleJournal of medicinal chemistry2013
Animal toxicity of hairpin pyrrole-imidazole polyamides varies with the turn unit.
Article in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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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
16 citing papers in PubMed, 34 citations in OpenAlex.
- Emerging Therapeutic Approaches to Engage the Androgen Receptor for the Treatment of Castration-Resistant Prostate Cancer.Cancers · 2025Review
- N-terminal domain of androgen receptor is a major therapeutic barrier and potential pharmacological target for treating castration resistant prostate cancer: a comprehensive review.Frontiers in pharmacology · 2024Review
- Targeting the mutant PIK3CA gene by DNA-alkylating pyrrole-imidazole polyamide in cervical cancer.Cancer science · 2021Article
- The Road Not Taken with Pyrrole-Imidazole Polyamides: Off-Target Effects and Genomic Binding.Biomolecules · 2020Review
- Sequence specific suppression of androgen receptor-DNA binding in vivo by a Py-Im polyamide.Nucleic acids research · 2019Article
- Molecules targeting the androgen receptor (AR) signaling axis beyond the AR-Ligand binding domain.Medicinal research reviews · 2019Review
- Estimating genome-wide off-target effects for pyrrole-imidazole polyamide binding by a pathway-based expression profiling approach.PloS one · 2019Article
- Structural basis of DNA duplex distortion induced by thiazole-containing hairpin polyamides.Nucleic acids research · 2018Article
- Interference with DNA repair after ionizing radiation by a pyrrole-imidazole polyamide.PloS one · 2018Article
- A Pyrrole-Imidazole Polyamide Is Active against Enzalutamide-Resistant Prostate Cancer.Cancer research · 2017Article
- [Recognition study of double strand DNA with hairpin oligopolyamide].Sheng wu yi xue gong cheng xue za zhi = Journal of biomedical engineering = Shengwu yixue gongchengxue zazhi · 2017Article
- Targeting NF-κB p65 with a Helenalin Inspired Bis-electrophile.ACS chemical biology · 2017Article
- An HRE-Binding Py-Im Polyamide Impairs Hypoxic Signaling in Tumors.Molecular cancer therapeutics · 2016Article
- Article
- Tumor xenograft uptake of a pyrrole-imidazole (Py-Im) polyamide varies as a function of cell line grafted.Journal of medicinal chemistry · 2014Article
- A C-14 labeled Py-Im polyamide localizes to a subcutaneous prostate cancer tumor.Bioorganic & medicinal chemistry · 2014Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
Abstract
A hairpin pyrrole-imidazole polyamide (1) targeted to the androgen receptor consensus half-site was found to exert antitumor effects against prostate cancer xenografts. A previous animal study showed that 1, which has a chiral amine at the α-position of the γ-aminobutyric acid turn (γ-turn), did not exhibit toxicity at doses less than 10 mg/kg. In the same study, a polyamide with an acetamide at the β-position of the γ-turn resulted in animal morbidity at 2.3 mg/kg. To identify structural motifs that cause animal toxicity, we synthesized polyamides 1-4 with variations at the α- and β-positions in the γ-turn. Weight loss, histopathology, and serum chemistry were analyzed in mice post-treatment. While serum concentration was similar for all four polyamides after injection, dose-limiting liver toxicity was only observed for three polyamides. Polyamide 3, with an α-acetamide, caused no significant evidence of rodent toxicity and retains activity against LNCaP xenografts.
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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.