ArticleProceedings of the National Academy of Sciences of the United States of America1999
Inhibition of gene expression in human cells through small molecule-RNA interactions.
Article in Proceedings of the National Academy of Sciences of the United States of America, 1999. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
22 citing papers in PubMed, 64 citations in OpenAlex.
- RNA Therapeutics in Viral Infections and Cancer: Mechanisms, Challenges, and Prospects: A Review.Pharmaceutics · 2026Review
- RNA-Binding Macrocyclic Peptides.Frontiers in molecular biosciences · 2022Review
- Molecular recognition of HIV-1 RNAs with branched peptides.Methods in enzymology · 2019Article
- Can the HIV-1 splicing machinery be targeted for drug discovery?HIV/AIDS (Auckland, N.Z.) · 2017Review
- Multivalency in the recognition and antagonism of a HIV TAR RNA-TAT assembly using an aminoglycoside benzimidazole scaffold.Organic & biomolecular chemistry · 2016Article
- Multivalent Amino Sugars to Recognize Different TAR RNA Conformations.MedChemComm · 2014Article
- Assessing specific oligonucleotides and small molecule antibiotics for the ability to inhibit the CRD-BP-CD44 RNA interaction.PloS one · 2014Article
- Selection of heptapeptides that bind helix 69 of bacterial 23S ribosomal RNA.Bioorganic & medicinal chemistry · 2013Article
- Click dimers to target HIV TAR RNA conformation.Biochemistry · 2012Article
- Toward targeting RNA structure: branched peptides as cell-permeable ligands to TAR RNA.ACS chemical biology · 2012Article
- Combinatorial Synthesis, Screening, and Binding Studies of Highly Functionalized Polyamino-amido Oligomers for Binding to Folded RNA.Journal of nucleic acids · 2012Article
- Recognition of HIV TAR RNA by triazole linked neomycin dimers.Bioorganic & medicinal chemistry letters · 2011Article
- A modified fluorescent intercalator displacement assay for RNA ligand discovery.Analytical biochemistry · 2011Article
- Nanotherapeutics Using an HIV-1 Poly A and Transactivator of the HIV-1 LTR-(TAR-) Specific siRNA.Pathology research international · 2011Article
- Selection of peptides that target the aminoacyl-tRNA site of bacterial 16S ribosomal RNA.Biochemistry · 2009Article
- Screening helix-threading peptides for RNA binding using a thiazole orange displacement assay.Bioorganic & medicinal chemistry · 2008Article
- Using an emissive uridine analogue for assembling fluorescent HIV-1 TAR constructs.Tetrahedron · 2007Article
- Conformational dynamics of RNA-peptide binding: a molecular dynamics simulation study.Biophysical journal · 2006Article
- Inhibition of human immunodeficiency virus type 1 tat-trans-activation-responsive region interaction by an antiviral quinolone derivative.Antimicrobial agents and chemotherapy · 2004Article
- New anti-human immunodeficiency virus type 1 6-aminoquinolones: mechanism of action.Antimicrobial agents and chemotherapy · 2003Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
Small molecules that bind their biological receptors with high affinity and selectivity can be isolated from randomized pools of combinatorial libraries. RNA-protein interactions are important in many cellular functions, including transcription, RNA splicing, and translation. One example of such interactions is the mechanism of trans-activation of HIV-1 gene expression that requires the interaction of Tat protein with the trans-activation responsive region (TAR) RNA, a 59-base stem-loop structure located at the 5' end of all nascent HIV-1 transcripts. Here we demonstrate the isolation of small TAR RNA-binding molecules from an encoded combinatorial library. We have made an encoded combinatorial tripeptide library of 24,389 possible members from D-and L-alpha amino acids on TentaGel resin. Using on-bead screening we have identified a small family of mostly heterochiral tripeptides capable of structure-specific binding to the bulge loop of TAR RNA. In vitro binding studies reveal stereospecific discrimination when the best tripeptide ligand is compared with diastereomeric peptide sequences. In addition, the most strongly binding tripeptide was shown to suppress transcriptional activation by Tat protein in human cells with an IC(50) of approximately 50 nM. Our results indicate that tripeptide RNA ligands are cell permeable, nontoxic to cells, and capable of inhibiting expression of specific genes by interfering with RNA-protein interactions.
Indexed as
Identifiers
What OpenQuestion holds
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.