ArticleAngewandte Chemie (International ed. in English)2020
Target-Directed Azide-Alkyne Cycloaddition for Assembling HIV-1 TAR RNA Binding Ligands.
Article in Angewandte Chemie (International ed. in English), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 30 citations in OpenAlex.
- A naturally occurring Tat R52W variant in brain-derived HIV attenuates transcription and may contribute to reservoir persistence.bioRxiv : the preprint server for biology · 2026Article
- Streamlined Fragment-Based Discovery Platform for Targeting Structured RNAs.ACS chemical biology · 2025Article
- A non-B DNA binding peptidomimetic channel alters cellular functions.Nature communications · 2024Article
- Small Molecules Targeting Viral RNA.International journal of molecular sciences · 2023Review
- Fragment-Based Approaches to Identify RNA Binders.Journal of medicinal chemistry · 2023Review
- HIV-1 Tat amino acid residues that influence Tat-TAR binding affinity: a scoping review.BMC infectious diseases · 2023Article
- Fragment-to-Lead Medicinal Chemistry Publications in 2020.Journal of medicinal chemistry · 2022Review
- A Novel Minor Groove Binder as a Potential Therapeutic Agent for Myotonic Dystrophy Type 1.ChemMedChem · 2021Article
- Design and Implementation of Synthetic RNA Binders for the Inhibition of miR-21 Biogenesis.ACS medicinal chemistry letters · 2021Article
- Target-Directed Azide-Alkyne Cycloaddition for Assembling HIV-1 TAR RNA Binding Ligands.Angewandte Chemie (International ed. in English) · 2020Article
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
The highly conserved HIV-1 transactivation response element (TAR) binds to the trans-activator protein Tat and facilitates viral replication in its latent state. The inhibition of Tat-TAR interactions by selectively targeting TAR RNA has been used as a strategy to develop potent antiviral agents. Therefore, HIV-1 TAR RNA represents a paradigmatic system for therapeutic intervention. Herein, we have employed biotin-tagged TAR RNA to assemble its own ligands from a pool of reactive azide and alkyne building blocks. To identify the binding sites and selectivity of the ligands, the in situ cycloaddition has been further performed using control nucleotide (TAR DNA and TAR RNA without bulge) templates. The hit triazole-linked thiazole peptidomimetic products have been isolated from the biotin-tagged target templates using streptavidin beads. The major triazole lead generated by the TAR RNA presumably binds in the bulge region, shows specificity for TAR RNA over TAR DNA, and inhibits Tat-TAR interactions.
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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.