Evidence map›Paper›PMID 34413954›Full record

ArticleACS medicinal chemistry letters2021

Efficient NMR Screening Approach to Discover Small Molecule Fragments Binding Structured RNA.

Matthew D Shortridge, Gabriele Varani

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.

0numbers the graph read from it
0cells of the map it votes in
13citing papers in PubMed
1.1field-weighted citation impact, top 23% 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

13 citing papers in PubMed, 21 citations in OpenAlex.

  1. Review
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  9. Article
  10. Fragment-Based Approaches to Identify RNA Binders.Journal of medicinal chemistry · 2023
    Review
  11. Review
  12. Article
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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

2 authors at 1 institution in 1 country.

Matthew D ShortridgeDepartment of Chemistry, University of Washington, Seattle, Washington 98195, United States.ORCID https://orcid.org/0000-0003-2825-6836
Gabriele VaraniDepartment of Chemistry, University of Washington, Seattle, Washington 98195, United States.
University of Washington · US

Funding

ncRNA: Structure, Interactions and InhibitionR35GM126942 · NIGMS · UNIVERSITY OF WASHINGTON · PI Gabriele Varani · 2018 to 2026
$6.0M
Regulation of microRNA processingR01GM103834 · NIGMS · UNIVERSITY OF WASHINGTON · PI VARANI, GABRIELE · 2014 to 2017
$1.1M
NIGMS NIH HHS R01 GM103834NIGMS NIH HHS R35 GM126942
6 · The paper itself

Abstract

We describe a scalable nuclear magnetic resonance (NMR) screening approach to identify and prioritize small molecule fragments that bind to structured RNAs. This approach is target agnostic and, therefore, amenable to many RNA structures and libraries, and it provides initial hits for further synthetic elaboration and structure-based drug discovery efforts. We demonstrate the approach on the pre-miR-21 stem-loop, which is of significant interest in oncology and metabolic diseases. We screened the pre-miR-21 hairpin using a small (420 compounds) commercially available fragment library and identified 18 hits in the first round of triage screening. This was further refined to four fragments which passed all screening cascade filters. Among these four hits, a thiadiazole fragment was demonstrated to bind the Dicer cleavage site of pre-miR-21 by target-detected NMR experiments and through the observation of clear intermolecular NOEs.

Identifiers

PMID34413954
PMCPMC8366005
OpenAlexW3177680647

What OpenQuestion holds

Textmetadata
Read underepoch 390

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.