ArticleBioorganic & medicinal chemistry letters2011
Anisotropy studies of tRNA-T box antiterminator RNA complex in the presence of 1,4-disubstituted 1,2,3-triazoles.
Article in Bioorganic & medicinal chemistry letters, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 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
7 citing papers in PubMed, 14 citations in OpenAlex.
- 4-Aminoquinolines modulate RNA structure and function: Pharmacophore implications of a conformationally restricted polyamine.Biochemical and biophysical research communications · 2023Article
- The T-Box Riboswitch: tRNA as an Effector to Modulate Gene Regulation.Microbiology spectrum · 2018Review
- Direct modulation of T-box riboswitch-controlled transcription by protein synthesis inhibitors.Nucleic acids research · 2017Article
- Identification of Spermidine Binding Site in T-box Riboswitch Antiterminator RNA.Chemical biology & drug design · 2016Article
- Factors that influence T box riboswitch efficacy and tRNA affinity.Bioorganic & medicinal chemistry · 2015Article
- Interfacing medicinal chemistry with structural bioinformatics: implications for T box riboswitch RNA drug discovery.BMC bioinformatics · 2012Article
- Ligand-induced changes in T box antiterminator RNA stability.Chemical biology & drug design · 2012Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
The binding of tRNA to the T box antiterminator RNA element is a critical component of the T box riboswitch mechanism that regulates essential genes in many Gram-positive bacteria. A series of 1,4-disubstituted 1,2,3-triazoles was screened for disruption of the tRNA-T box antiterminator RNA interaction using a fluorescence anisotropy-based assay. Several compounds reduced the anisotropy greater than 50% likely indicating significant competition for binding antiterminator RNA. General structure-activity trends indicated that the substituents at both N-1 and C-4 likely are involved in ligand binding. In addition, the anisotropy of the complex was significantly decreased not only by ligands with the possibility for electrostatic interactions with the RNA, but also by ligands with the potential for π-π stacking or other hydrophobic interactions indicating that these non-electrostatic interactions could possibly be utilized in the future development of compounds that target and disrupt the function of this medicinally important riboswitch.
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Registered trials
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