Evidence map›Paper›PMID 30251629›Full record

ArticleCell chemical biology2018

Approved Anti-cancer Drugs Target Oncogenic Non-coding RNAs.

Sai Pradeep Velagapudi, Matthew G Costales, Balayeshwanth R Vummidi, Yoshio Nakai, Alicia J Angelbello, Tuan Tran, Hafeez S Haniff, Yasumasa Matsumoto, Zi Fu Wang, Arnab K Chatterjee and 2 more

Open access · bronzeAbstract read
In one paragraph

Article in Cell chemical biology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 57 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
57citing papers in PubMed, 1 pooled it
4.0field-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

57 citing papers in PubMed, 1 synthesis or guideline pooled it, 79 citations in OpenAlex.

  1. Pooled it
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  17. Fragment-Based Approaches to Identify RNA Binders.Journal of medicinal chemistry · 2023
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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

12 authors at 2 institutions in 1 country.

Sai Pradeep VelagapudiDepartment of Chemistry, The Scripps Research Institute, 130 Scripps Way, Jupiter, FL 33458, USA.
Matthew G CostalesDepartment of Chemistry, The Scripps Research Institute, 130 Scripps Way, Jupiter, FL 33458, USA.
Balayeshwanth R VummidiDepartment of Chemistry, The Scripps Research Institute, 130 Scripps Way, Jupiter, FL 33458, USA.
Yoshio NakaiDepartment of Chemistry, The Scripps Research Institute, 130 Scripps Way, Jupiter, FL 33458, USA.
Alicia J AngelbelloDepartment of Chemistry, The Scripps Research Institute, 130 Scripps Way, Jupiter, FL 33458, USA.
Tuan TranDepartment of Chemistry, The Scripps Research Institute, 130 Scripps Way, Jupiter, FL 33458, USA.
Hafeez S HaniffDepartment of Chemistry, The Scripps Research Institute, 130 Scripps Way, Jupiter, FL 33458, USA.
Yasumasa MatsumotoDepartment of Chemistry, The Scripps Research Institute, 130 Scripps Way, Jupiter, FL 33458, USA.
Zi Fu WangDepartment of Chemistry, The Scripps Research Institute, 130 Scripps Way, Jupiter, FL 33458, USA.
Arnab K ChatterjeeCalifornia Institute for Biomedical Research (CALIBR), 11119 North Torrey Pines Road, Suite 100, La Jolla, CA 92037, USA.
Jessica L Childs-DisneyDepartment of Chemistry, The Scripps Research Institute, 130 Scripps Way, Jupiter, FL 33458, USA.
Matthew D DisneyDepartment of Chemistry, The Scripps Research Institute, 130 Scripps Way, Jupiter, FL 33458, USA. Electronic address: disney@scripps.edu.
Scripps Research Institute · USCalifornia Institute for Biomedical Research · US

Funding

Sequence-based Design of Small Molecules Targeting RNAR01GM097455 · NIGMS · SCRIPPS FLORIDA · PI DISNEY, MATTHEW D · 2012 to 2019
$4.6M
NIGMS NIH HHS R01 GM097455
6 · The paper itself

Abstract

Potential RNA drug targets for small molecules are found throughout the human transcriptome, yet small molecules known to elicit a pharmacological response by directly targeting RNA are limited to antibacterials. Herein, we describe AbsorbArray, a small molecule microarray-based approach that allows for unmodified compounds, including FDA-approved drugs, to be probed for binding to RNA motif libraries in a massively parallel format. Several drug classes bind RNA including kinase and topoisomerase inhibitors. The latter avidly bound the motif found in the Dicer site of oncogenic microRNA (miR)-21 and inhibited its processing both in vitro and in cells. The most potent compound de-repressed a downstream protein target and inhibited a miR-21-mediated invasive phenotype. The compound's activity was ablated upon overexpression of pre-miR-21. Target validation via chemical crosslinking and isolation by pull-down showed direct engagement of pre-miR-21 by the small molecule in cells, demonstrating that RNAs should indeed be considered druggable.

Indexed as

Drug DesignAntineoplastic AgentsCell Line, TumorDrug ApprovalDrug DiscoveryHumansMicroRNAsMolecular Targeted TherapyNeoplasmsSmall Molecule LibrariesAntineoplastic AgentsMicroRNAsMIRN21 microRNA, humanSmall Molecule Librariescancerchemical biologynon-coding RNAsnucleic acidsrational designRNAsmall molecules

Identifiers

PMID30251629
PMCPMC6334646
OpenAlexW2810410733

What OpenQuestion holds

Textmetadata
LicenceTDM
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.