ArticleNucleic acids research2000
Specific binding of Hoechst 33258 to site 1 thymidylate synthase mRNA.
Article in Nucleic acids research, 2000. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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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
21 citing papers in PubMed, 48 citations in OpenAlex.
- Targeting Expanded CUG and CTG Repeats as a Therapeutic Approach for Myotonic Dystrophy Type 1 (DM1).ChemMedChem · 2026Review
- Discovery of RNA-Reactive Small Molecules Guides the Design of Electrophilic Modules for RNA-Specific Covalent Binders.Journal of the American Chemical Society · 2025Article
- Targeting RNA with small molecules, from RNA structures to precision medicines: IUPHAR review: 40.British journal of pharmacology · 2024Review
- Enhanced visualization of nuclear staining and cell cycle analysis for the human commensal Malassezia.Scientific reports · 2024Article
- Contemporary Progress and Opportunities in RNA-Targeted Drug Discovery.ACS medicinal chemistry letters · 2023Review
- Insights into the development of chemical probes for RNA.Nucleic acids research · 2018Article
- Studying a Drug-like, RNA-Focused Small Molecule Library Identifies Compounds That Inhibit RNA Toxicity in Myotonic Dystrophy.ACS chemical biology · 2015Article
- Versatile on-resin synthesis of high mannose glycosylated asparagine with functional handles.Carbohydrate research · 2014Article
- MBNL proteins and their target RNAs, interaction and splicing regulation.Nucleic acids research · 2014Review
- Rational design of chemical genetic probes of RNA function and lead therapeutics targeting repeating transcripts.Drug discovery today · 2013Review
- Translational repression of thymidylate synthase by targeting its mRNA.Nucleic acids research · 2013Article
- H-gemcitabine: a new gemcitabine prodrug for treating cancer.Bioconjugate chemistry · 2013Article
- Pyrrole-imidazole polyamides distinguish between double-helical DNA and RNA.Angewandte Chemie (International ed. in English) · 2013Article
- Targeting a regulatory element in human thymidylate synthase mRNA.Chembiochem : a European journal of chemical biology · 2012Article
- A small molecule that targets r(CGG)(exp) and improves defects in fragile X-associated tremor ataxia syndrome.ACS chemical biology · 2012Article
- Identifying the preferred RNA motifs and chemotypes that interact by probing millions of combinations.Nature communications · 2012Article
- Using modularly assembled ligands to bind RNA internal loops separated by different distances.Chembiochem : a European journal of chemical biology · 2011Article
- Defining the RNA internal loops preferred by benzimidazole derivatives via 2D combinatorial screening and computational analysis.Journal of the American Chemical Society · 2011Article
- Rational design of ligands targeting triplet repeating transcripts that cause RNA dominant disease: application to myotonic muscular dystrophy type 1 and spinocerebellar ataxia type 3.Journal of the American Chemical Society · 2009Article
- Rational selection of small molecules that increase transcription through the GAA repeats found in Friedreich's ataxia.FEBS letters · 2006Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
The translational initiator codon in thymidylate synthetase (TS) mRNA is located in a stem-loop structure with a CC bubble. TS is an important target for anticancer drugs. Aminoglycoside antibiotics have been shown to specifically bind to TS mRNA site 1 constructs and, furthermore, specific binding requires the non-duplex CC bubble region. It is shown here that DNA intercalating agents and DNA minor groove-binding drugs also bind to a TS mRNA site 1 construct. This binding is competitive with aminoglycosides, suggesting that the binding sites overlap. Hoechst 33258 binds with a dissociation constant of 60 nM, a value significantly lower than the approximately 1 microM values found for aminoglycosides. Footprinting and direct binding studies show that the CC bubble is important for binding of the Hoechst compound. However, the exact structure of the bubble is unimportant. Interestingly, mutations in regions adjacent to the bulge also affect binding. These studies point to the important role of non-duplex RNA structures in binding of the DNA minor groove binder Hoechst 33258.
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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.