Evidence map›Paper›PMID 31912579›Full record

ReviewCancer science2020

Discovery of chemical probes that suppress Wnt/β-catenin signaling through high-throughput screening.

Kiyoshi Yamaguchi, Satoru Nagatoishi, Kouhei Tsumoto, Yoichi Furukawa

Open access · goldAbstract readReview
In one paragraph

Review in Cancer science, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
0.8field-weighted citation impact, top 31% 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

11 citing papers in PubMed, 14 citations in OpenAlex.

  1. Review
  2. Cis-regulatory control of mammalian Trps1 gene expression.Journal of experimental zoology. Part B, Molecular and developmental evolution · 2024
    Article
  3. Article
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  7. Review
  8. Article
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  11. 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

4 authors at 1 institution in 1 country.

Kiyoshi YamaguchiDivision of Clinical Genome Research, Advanced Clinical Research Center, Institute of Medical Science, The University of Tokyo, Tokyo, Japan.ORCID https://orcid.org/0000-0003-2113-4369
Satoru NagatoishiProject Division of Advanced Biopharmaceutical Science, Institute of Medical Science, The University of Tokyo, Tokyo, Japan.
Kouhei TsumotoProject Division of Advanced Biopharmaceutical Science, Institute of Medical Science, The University of Tokyo, Tokyo, Japan.
Yoichi FurukawaDivision of Clinical Genome Research, Advanced Clinical Research Center, Institute of Medical Science, The University of Tokyo, Tokyo, Japan.ORCID https://orcid.org/0000-0003-0462-8631
The University of Tokyo · JP

Funding

Japan Agency for Medical Research and Development, AMEDJapan Society for the Promotion of SciencePlatform Project for Supporting Drug Discovery and Life Science Research (Basis for Supporting Innovative Drug Discovery and Life Science Research (BINDS)) from AMED of Japan JP19am0101094Takeda Science Foundation
6 · The paper itself

Abstract

Aberrant activation of the Wnt/β-catenin signaling pathway has been observed in a wide range of human tumors. Deregulation of the pathway is closely linked to various aspects of human carcinogenesis such as cell viability, regulation of cell cycle, epithelial-mesenchymal transition, and maintenance of stemness. In addition, recent studies have disclosed the involvement of Wnt signaling in immune evasion of tumor cells. The accumulation of β-catenin in the nucleus is a common feature of cancer cells carrying defects in the pathway, which leads to the continuous activation of T-cell factor (TCF)/LEF transcription factors. Consequently, a genetic program is switched on, leading to the uncontrolled growth, prolonged survival, and acquisition of mesenchymal phenotype. As β-catenin/TCF serves as a signaling hub for the pathway, β-catenin/TCF-dependent transcriptional activity is a relevant readout of the pathway. To date, a wide variety of synthetic TCF/LEF reporters has been developed, and high-throughput screening (HTS) using these reporters has made significant contributions to the discovery of Wnt inhibitors. Indeed, HTS led to the identification of chemical probes targeting porcupine, a membrane bound O-acyltransferase, and CREB-binding protein, a transcriptional coactivator. This review focuses on various screening strategies for the discovery of Wnt inhibitors and their mode of action to help the creation of new concepts for assay/screening methods.

Indexed as

AnimalsAntineoplastic Agentsbeta CateninHigh-Throughput Screening AssaysHumansTranscription FactorsWnt Signaling PathwayAntineoplastic Agentsbeta CateninCTNNB1 protein, humanTranscription Factorschemical probehigh-throughput screeningreporter assayTCF/LEF transcription factorWnt/β-catenin signaling pathway

Identifiers

PMID31912579
PMCPMC7060471
OpenAlexW2999676366

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC
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.