Evidence map›Paper›PMID 38784453›Full record

ArticleRSC medicinal chemistry2024

Live cell screening to identify RNA-binding small molecule inhibitors of the pre-let-7-Lin28 RNA-protein interaction.

Sydney L Rosenblum, Dalia M Soueid, George Giambasu, Steve Vander Roest, Alexander Pasternak, Erin F DiMauro, Vladimir Simov, Amanda L Garner

Abstract read
In one paragraph

Article in RSC medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing 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

4 citing papers in PubMed.

  1. Review
  2. Article
  3. Review
  4. 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

8 authors.

Sydney L RosenblumProgram in Chemical Biology, University of Michigan 210 Washtenaw Avenue Ann Arbor MI 48109 USA algarner@umich.edu.ORCID https://orcid.org/0000-0001-8231-6559
Dalia M SoueidDepartment of Medicinal Chemistry, College of Pharmacy, University of Michigan 1600 Huron Parkway, NCRC B520 Ann Arbor MI 48109 USA.
George GiambasuComputational Chemistry, Merck & Co., Inc. Boston MA 02115 USA george.giambasu@merck.com.ORCID https://orcid.org/0000-0003-0581-8605
Steve Vander RoestCenter for Chemical Genomics, Life Sciences Institute, University of Michigan 210 Washtenaw Avenue Ann Arbor MI 48109 USA.
Alexander PasternakDiscovery Chemistry, Merck & Co., Inc. Boston MA 02115 USA alexander_pasternak@merck.com erin.dimauro@merck.com vladimir_simov@merck.com.
Erin F DiMauroDiscovery Chemistry, Merck & Co., Inc. Boston MA 02115 USA alexander_pasternak@merck.com erin.dimauro@merck.com vladimir_simov@merck.com.
Vladimir SimovDiscovery Chemistry, Merck & Co., Inc. Boston MA 02115 USA alexander_pasternak@merck.com erin.dimauro@merck.com vladimir_simov@merck.com.ORCID https://orcid.org/0000-0002-6068-1894
Amanda L GarnerProgram in Chemical Biology, University of Michigan 210 Washtenaw Avenue Ann Arbor MI 48109 USA algarner@umich.edu.ORCID https://orcid.org/0000-0002-0870-3347

Funding

Cellular Biotechnology Training Program (CBTP) - Years 31-35T32GM145304 · NIGMS · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI Guizhi Zhu · 2022 to 2026
$2.6M
Chemical Biology Approach for Validating and Manipulating Cellular RNA-Protein InteractionsR01GM135252 · NIGMS · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI GARNER, AMANDA · 2019 to 2022
$1.4M
NIGMS NIH HHS R01 GM135252NIGMS NIH HHS T32 GM145304
6 · The paper itself

Abstract

Dysregulation of the networking of RNA-binding proteins (RBPs) and RNAs drives many human diseases, including cancers, and the targeting of RNA-protein interactions (RPIs) has emerged as an exciting area of RNA-targeted drug discovery. Accordingly, methods that enable the discovery of cell-active small molecule modulators of RPIs are needed to propel this emerging field forward. Herein, we describe the application of live-cell assay technology, RNA interaction with protein-mediated complementation assay (RiPCA), for high-throughput screening to identify small molecule inhibitors of the pre-let-7d-Lin28A RPI. Utilizing a combination of RNA-biased small molecules and virtual screening hits, we discovered an RNA-binding small molecule that can disrupt the pre-let-7-Lin28 interaction demonstrating the potential of RiPCA for advancing RPI-targeted drug discovery.

Identifiers

PMID38784453
PMCPMC11110735

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Registered trials

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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.