Evidence map›Paper›PMID 37312841›Full record

ArticleACS medicinal chemistry letters2023

Development of DNA Aptamer-Based PROTACs That Degrade the Estrogen Receptor.

Haruna Tsujimura, Miyako Naganuma, Nobumichi Ohoka, Takao Inoue, Mikihiko Naito, Genichiro Tsuji, Yosuke Demizu

Abstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing 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

9 citing papers in PubMed.

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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

7 authors.

Haruna TsujimuraDivision of Organic Chemistry, National Institute of Health Sciences, Kanagawa 210-9501, Japan.
Miyako NaganumaDivision of Organic Chemistry, National Institute of Health Sciences, Kanagawa 210-9501, Japan.
Nobumichi OhokaDivision of Molecular Target and Gene Therapy Products, National Institute of Health Sciences, Kanagawa 210-9501, Japan.ORCID https://orcid.org/0000-0002-0533-0610
Takao InoueDivision of Molecular Target and Gene Therapy Products, National Institute of Health Sciences, Kanagawa 210-9501, Japan.
Mikihiko NaitoLaboratory of Targeted Protein Degradation, Graduate School of Pharmaceutical Sciences, The University of Tokyo, Tokyo 113-0033, Japan.ORCID https://orcid.org/0000-0003-0451-1337
Genichiro TsujiDivision of Organic Chemistry, National Institute of Health Sciences, Kanagawa 210-9501, Japan.ORCID https://orcid.org/0000-0002-2826-3852
Yosuke DemizuDivision of Organic Chemistry, National Institute of Health Sciences, Kanagawa 210-9501, Japan.ORCID https://orcid.org/0000-0001-7521-4861

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Targeted protein degradation (TPD), using chimeric molecules such as proteolysis-targeting chimeras (PROTACs), has attracted attention as a strategy for selective degradation of intracellular proteins by hijacking the ubiquitin-proteasome system (UPS). However, it is often difficult to develop such degraders due to the absence of appropriate ligands for target proteins. In targeting proteins for degradation, the application of nucleic acid aptamers is considered to be effective because these can be explored using systematic evolution of ligand by exponential enrichment (SELEX) methods. In this study, we constructed chimeric molecules in which nucleic acid aptamers capable of binding to the estrogen receptor α (ERα) and E3 ubiquitin ligase ligands were linked via a linker. ERα aptamer-based PROTACs were found to degrade ERα via the UPS. These findings represent the development of novel aptamer-based PROTACs that target intracellular proteins and are potentially applicable to other proteins.

Identifiers

PMID37312841
PMCPMC10258903

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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.