Evidence map›Paper›PMID 26765486›Full record

ArticleOrganic & biomolecular chemistry2016

Multivalency in the recognition and antagonism of a HIV TAR RNA-TAT assembly using an aminoglycoside benzimidazole scaffold.

Sunil Kumar, Nihar Ranjan, Patrick Kellish, Changjun Gong, Derrick Watkins, Dev P Arya

Abstract read
In one paragraph

Article in Organic & biomolecular chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.

0numbers the graph read from it
0cells of the map it votes in
19citing papers in PubMed
–field-weighted citation impact
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

19 citing papers in PubMed.

  1. Article
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  6. Small molecule-RNA targeting: starting with the fundamentals.Chemical communications (Cambridge, England) · 2020
    Article
  7. Article
  8. Article
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  15. Article
  16. Small Molecule-Based Pattern Recognition To Classify RNA Structure.Journal of the American Chemical Society · 2017
    Article
  17. Article
  18. Small molecules targeting viral RNA.Wiley interdisciplinary reviews. RNA · 2016
    Review
  19. Frameworks for targeting RNA with small molecules.The Journal of biological chemistry
    Review
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

6 authors.

Sunil KumarLaboratory of Medicinal Chemistry, Department of Chemistry, Clemson University, Clemson, SC 29634, USA. dparya@clemson.edu.
Nihar RanjanLaboratory of Medicinal Chemistry, Department of Chemistry, Clemson University, Clemson, SC 29634, USA. dparya@clemson.edu and Nubad LLC, 900 B West Faris Road, Greenville, SC 29630, USA.
Patrick KellishLaboratory of Medicinal Chemistry, Department of Chemistry, Clemson University, Clemson, SC 29634, USA. dparya@clemson.edu.
Changjun GongLaboratory of Medicinal Chemistry, Department of Chemistry, Clemson University, Clemson, SC 29634, USA. dparya@clemson.edu.
Derrick WatkinsNubad LLC, 900 B West Faris Road, Greenville, SC 29630, USA.
Dev P AryaLaboratory of Medicinal Chemistry, Department of Chemistry, Clemson University, Clemson, SC 29634, USA. dparya@clemson.edu.

Funding

A Rapid assay for RNA targeted drugs: Instrumentation SupplementR42GM097917 · NIGMS · NUBAD, LLC · PI ARYA, DEV PRIYA · 2014 to 2015
$1.4M
Development of Ets2-InhibitorsR15CA125724 · NCI · CLEMSON UNIVERSITY · PI ARYA, DEV PRIYA · 2008 to 2009
$398k
A novel assay for RNA targeted drugsR41GM097917 · NIGMS · NUBAD, LLC · PI ARYA, DEV PRIYA · 2011 to 2011
$286k
NCI NIH HHS R15 CA125724NCI NIH HHS R15CA125724NIGMS NIH HHS GM097917NIGMS NIH HHS R41 GM097917NIGMS NIH HHS R42 GM097917
6 · The paper itself

Abstract

Recognition of RNA by high-affinity binding small molecules is crucial for expanding existing approaches in RNA recognition, and for the development of novel RNA binding drugs. A novel neomycin dimer benzimidazole conjugate 5 (DPA 83) was synthesized by conjugating a neomycin-dimer with a benzimidazole alkyne using click chemistry to target multiple binding sites on HIV TAR RNA. Ligand 5 significantly enhances the thermal stability of HIV TAR RNA and interacts stoichiometrically with HIV TAR RNA with a low nanomolar affinity. 5 displayed enhanced binding compared to its individual building blocks including the neomycin dimer azide and benzimidazole alkyne. In essence, a high affinity multivalent ligand was designed and synthesized to target HIV TAR RNA.

Indexed as

AminoglycosidesBenzimidazolesBinding SitesClick ChemistryDose-Response Relationship, DrugHIV Long Terminal RepeatLigandsMolecular ConformationNeomycinRNA, ViralStructure-Activity RelationshipAminoglycosidesbenzimidazoleBenzimidazolesLigandsNeomycinRNA, Viral

Identifiers

PMID26765486
PMCPMC4837457

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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.