Evidence map›Paper›PMID 26820295›Full record

ArticleOncotarget2016

Identification of quinazoline compounds as novel potent inhibitors of Wnt/β-catenin signaling in colorectal cancer cells.

Yonghe Li, Wenyan Lu, Surendra K Saini, Omar Moukha-Chafiq, Vibha Pathak, Subramaniam Ananthan

Open access · diamondAbstract read
In one paragraph

Article in Oncotarget, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing papers in PubMed
1.2field-weighted citation impact, top 20% 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

10 citing papers in PubMed, 16 citations in OpenAlex.

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  7. New dinuclear palladium(II) complexes with benzodiazines as bridging ligands: interactions with CT-DNA and BSA, and cytotoxic activity.Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry · 2019
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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.

Yonghe LiDrug Discovery Division, Southern Research Institute, Birmingham, AL 35205, United States of America.
Wenyan LuDrug Discovery Division, Southern Research Institute, Birmingham, AL 35205, United States of America.
Surendra K SainiDrug Discovery Division, Southern Research Institute, Birmingham, AL 35205, United States of America.
Omar Moukha-ChafiqDrug Discovery Division, Southern Research Institute, Birmingham, AL 35205, United States of America.
Vibha PathakDrug Discovery Division, Southern Research Institute, Birmingham, AL 35205, United States of America.
Subramaniam AnanthanDrug Discovery Division, Southern Research Institute, Birmingham, AL 35205, United States of America.
Southern Research Institute · US

Funding

Wnt co-receptor LRP6 turnover and cancerR01CA124531 · NCI · SOUTHERN RESEARCH INSTITUTE · PI LI, YONGHE · 2008 to 2011
$1.9M
Targeted Library Synthesis and Screening: Allosteric Modulators of TransportersR33DA029962 · NIDA · SOUTHERN RESEARCH INSTITUTE · PI ANANTHAN, SUBRAMANIAM · 2012 to 2014
$1.2M
Targeted Library Synthesis and Screening: Allosteric Modulators of TransportersR21DA029962 · NIDA · SOUTHERN RESEARCH INSTITUTE · PI ANANTHAN, SUBRAMANIAM · 2010 to 2011
$757k
Small molecule Fzd7 inhibitors for cancer therapyR21CA182056 · NCI · SOUTHERN RESEARCH INSTITUTE · PI LI, YONGHE · 2014 to 2015
$571k
NCI NIH HHS R01 CA124531NCI NIH HHS R21 CA182056NIDA NIH HHS R33 DA029962
6 · The paper itself

Abstract

The Wnt/β-catenin signaling pathway is critical for the initiation and progression of most colon cancers, and has emerged as one of the most promising targets for colorectal cancer chemoprevention and treatment. In this study, we have discovered a structurally related series of quinazolines as potent inhibitors of Wnt/β-catenin signaling in colorectal cancer cells harboring mutations in CTNNB1 or APC. We showed that the quinazoline leads suppressed Wnt/β-catenin signaling without altering the level of β-catenin protein in colorectal cancer cells, suggesting that they act on the downstream elements of the pathway. Moreover, the quinazoline leads displayed potent anticancer activities with IC50 values between 4.9 and 17.4 μM in colorectal cancer cells. Importantly, we also found that a structurally related quinazoline lacking inhibitory effect on Wnt/β-catenin signaling was unable to suppress colorectal cancer cell proliferation. Together, these results suggest that the quinazoline lead compounds identified in this study have therapeutic potential for the prevention and treatment of colorectal cancer.

Indexed as

Antineoplastic AgentsCell Line, TumorCell ProliferationColorectal NeoplasmsDrug Screening Assays, AntitumorHumansInhibitory Concentration 50QuinazolinesWnt Signaling PathwayAntineoplastic AgentsQuinazolinescolorectal cancerdrug discoveryquinazolineWnt inhibitorWnt signaling

Identifiers

PMID26820295
PMCPMC4905471
OpenAlexW2296659812

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.