Evidence map›Paper›PMID 28002966›Full record

ArticleJournal of medicinal chemistry2016

Development of Small Molecules with a Noncanonical Binding Mode to HIV-1 Trans Activation Response (TAR) RNA.

Fardokht A Abulwerdi, Matthew D Shortridge, Joanna Sztuba-Solinska, Robert Wilson, Stuart F J Le Grice, Gabriele Varani, John S Schneekloth

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 52 papers.

0numbers the graph read from it
0cells of the map it votes in
52citing papers in PubMed
4.7field-weighted citation impact, top 5% of its field
1 · What the graph read from it

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.

2 · The registry

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.

3 · Its place in the literature

Who cites it

52 citing papers in PubMed, 87 citations in OpenAlex.

  1. Article
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  10. Identification of RNA structures and their roles in RNA functions.Nature reviews. Molecular cell biology · 2024
    Review
  11. Article
  12. Review
  13. HIV-1 Transcription Inhibition Using Small RNA-Binding Molecules.Pharmaceuticals (Basel, Switzerland) · 2023
    Article
  14. Review
  15. Article
  16. Targeting RNA structures with small molecules.Nature reviews. Drug discovery · 2022
    Review
  17. Review
  18. Article
  19. Article
  20. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

7 authors at 2 institutions in 1 country.

Fardokht A AbulwerdiChemical Biology Laboratory, National Cancer Institute , 376 Boyles Street, Room 225C, Frederick, Maryland 21702, United States.
Matthew D ShortridgeDepartment of Chemistry, University of Washington , Seattle, Washington 98195, United States.
Joanna Sztuba-SolinskaBasic Research Laboratories, National Cancer Institute , Frederick, Maryland 21702, United States.
Robert WilsonChemical Biology Laboratory, National Cancer Institute , 376 Boyles Street, Room 225C, Frederick, Maryland 21702, United States.
Stuart F J Le GriceBasic Research Laboratories, National Cancer Institute , Frederick, Maryland 21702, United States.
Gabriele VaraniDepartment of Chemistry, University of Washington , Seattle, Washington 98195, United States.
John S SchneeklothChemical Biology Laboratory, National Cancer Institute , 376 Boyles Street, Room 225C, Frederick, Maryland 21702, United States.ORCID 0000-0001-7459-783X
Frederick National Laboratory for Cancer Research · USUniversity of Washington · US

Funding

Identification of Nucleic Acid Binding Small MoleculesZIABC011585 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI SCHNEEKLOTH, JOHN · 2014 to 2025
$18.6M
New Inhibitors of HIV replicationR01GM110569 · NIGMS · UNIVERSITY OF WASHINGTON · PI KARN, JONATHAN, VARANI, GABRIELE · 2013 to 2016
$1.7M
NIGMS NIH HHS R01 GM110569
6 · The paper itself

Abstract

Small molecules that bind to RNA potently and specifically are relatively rare. The study of molecules that bind to the HIV-1 transactivation response (TAR) hairpin, a cis-acting HIV genomic element, has long been an important model system for the chemistry of targeting RNA. Here we report the synthesis, biochemical, and structural evaluation of a series of molecules that bind to HIV-1 TAR RNA. A promising analogue, 15, retained the TAR binding affinity of the initial hit and displaced a Tat-derived peptide with an IC

Indexed as

Binding SitesDose-Response Relationship, DrugHIV Long Terminal RepeatMolecular StructureRNA, ViralSmall Molecule LibrariesStructure-Activity RelationshipTranscriptional ActivationRNA, ViralSmall Molecule Libraries

Identifiers

PMID28002966
PMCPMC5525537
OpenAlexW2552845674

What OpenQuestion holds

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Registered trials

None linked

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.