Evidence map›Paper›PMID 37870980›Full record

ArticleACS chemical biology2023

Optimization of a Protein-Targeted Medicine into an RNA-Specific Small Molecule.

Samantha M Meyer, Toru Tanaka, Amirhossein Taghavi, Jared T Baisden, Maison Grefe, Matthew D Disney

Open access · greenAbstract read
In one paragraph

Article in ACS chemical biology, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
1.2field-weighted citation impact, top 24% 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

6 citing papers in PubMed, 8 citations in OpenAlex.

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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

6 authors at 1 institution in 1 country.

Samantha M MeyerThe Herbert Wertheim UF Scripps Institute for Biomedical Innovation and Technology, Department of Chemistry, 130 Scripps Way, Jupiter, Florida 33458 United States.ORCID 0000-0003-3353-6939
Toru TanakaThe Herbert Wertheim UF Scripps Institute for Biomedical Innovation and Technology, Department of Chemistry, 130 Scripps Way, Jupiter, Florida 33458 United States.
Amirhossein TaghaviThe Herbert Wertheim UF Scripps Institute for Biomedical Innovation and Technology, Department of Chemistry, 130 Scripps Way, Jupiter, Florida 33458 United States.
Jared T BaisdenThe Scripps Research Institute, Department of Chemistry, 130 Scripps Way, Jupiter, Florida 33458 United States.
Maison GrefeThe Scripps Research Institute, Department of Chemistry, 130 Scripps Way, Jupiter, Florida 33458 United States.
Matthew D DisneyThe Herbert Wertheim UF Scripps Institute for Biomedical Innovation and Technology, Department of Chemistry, 130 Scripps Way, Jupiter, Florida 33458 United States.ORCID 0000-0001-8486-1796
Scripps Research Institute · US

Funding

Targeted degradation of RNAs by using small moleculesR01CA249180 · NCI · UNIVERSITY OF FLORIDA · PI Matthew D Disney · 2020 to 2026
$4.8M
Bruker Avance III HD 600 MHz NMR spectrometerS10OD021550 · OD · SCRIPPS FLORIDA · PI KOJETIN, DOUGLAS · 2017 to 2017
$600k
NCI NIH HHS R01 CA249180NIH HHS S10 OD021550
6 · The paper itself

Abstract

Protein-targeted small molecule medicines often bind RNAs and affect RNA-mediated pathways in cells. Historically, small molecule engagement and modulation of RNA have not been considered in medicine development; however, RNA should be considered both a potential on- and off-target. Kinase inhibitors have emecrged as common RNA binders with dovitinib, a classic receptor tyrosine kinase (RTK) inhibitor, inhibiting RTKs and the biogenesis of oncogenic microRNA-21 through direct engagement. In this study, we use knowledge of the molecular recognition of both protein and RNA targets by dovitinib to design molecules that specifically inhibit the RNA target but lack activity against canonical protein targets in cells. As it is now becoming apparent that RNA can be both an on- and off-target for small molecule medicines, this study lays a foundation to use design principles to maximize desired compound activity while minimizing off-target effects.

Indexed as

MicroRNAsProtein Kinase InhibitorsReceptor Protein-Tyrosine KinasesMicroRNAsProtein Kinase InhibitorsReceptor Protein-Tyrosine Kinases

Identifiers

PMID37870980
PMCPMC10825933
OpenAlexW4387873555

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.