Evidence map›Paper›PMID 31684051›Full record

ArticleJournal of clinical medicine2019

Development of Oxadiazole-Based ODZ10117 as a Small-Molecule Inhibitor of STAT3 for Targeted Cancer Therapy.

Byung-Hak Kim, Haeri Lee, Yeonghun Song, Joon-Suk Park, Changdev G Gadhe, Jiwon Choi, Chung-Gi Lee, Ae Nim Pae, Sanghee Kim, Sang-Kyu Ye

Open access · goldAbstract read
In one paragraph

Article in Journal of clinical medicine, 2019. 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
1.0field-weighted citation impact, top 21% 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, 19 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

10 authors at 3 institutions in 1 country.

Byung-Hak KimDepartment of Pharmacology and Biomedical Sciences, Seoul National University College of Medicine, Seoul 03080, Korea. protein0826@snu.ac.kr.
Haeri LeeDepartment of Pharmacology and Biomedical Sciences, Seoul National University College of Medicine, Seoul 03080, Korea. hrlee519@snu.ac.kr.
Yeonghun SongCollege of Pharmacy, Seoul National University, Seoul 08826, Korea. song2@snu.ac.kr.
Joon-Suk ParkLaboratory Animal Center, Daegu-Gyeongbuk Medical Innovation Foundation, Daegu 41061, Korea. song2@snu.ac.kr.
Changdev G GadheConvergence Research Center for Diagnosis, Treatment and Care System of Dementia, Korea Institute of Science and Technology, Seoul 02792, Korea. gadhe.changdev@gmail.com.
Jiwon ChoiDepartment of Pharmacology and Biomedical Sciences, Seoul National University College of Medicine, Seoul 03080, Korea. c_jiwon@hotmail.com.
Chung-Gi LeeCYTUS H&B Corporation, Cheongju 28159, Korea. cglee2020@gmail.com.
Ae Nim PaeConvergence Research Center for Diagnosis, Treatment and Care System of Dementia, Korea Institute of Science and Technology, Seoul 02792, Korea. anpae@kist.re.kr.
Sanghee KimCollege of Pharmacy, Seoul National University, Seoul 08826, Korea. pennkim@snu.ac.kr.
Sang-Kyu YeDepartment of Pharmacology and Biomedical Sciences, Seoul National University College of Medicine, Seoul 03080, Korea. sangkyu@snu.ac.kr.
Seoul National University · KRConvergence Research Center for Diagnosis Treatment and Care System of Dementia · KRDaegu-Gyeongbuk Medical Innovation Foundation · KR

Funding

Cooperative Research Program of Basic Medical Science and Clinical Science from Seoul National University College of Medicine 800-20160092the Basic Science Research Program through the National Research Foundation of Korea 2016R1D1A1B03931766the National Research Foundation of Korea 2017R1A2B2006839
6 · The paper itself

Abstract

Persistently activated STAT3 is a promising target for a new class of anticancer drug development and cancer therapy, as it is associated with tumor initiation, progression, malignancy, drug resistance, cancer stem cell properties, and recurrence. Here, we discovered 3-(2,4-dichloro-phenoxymethyl)-5-trichloromethyl-[1,2,4]oxadiazole (ODZ10117) as a small-molecule inhibitor of STAT3 to be used in STAT3-targeted cancer therapy. ODZ10117 targeted the SH2 domain of STAT3 regardless of other STAT family proteins and upstream regulators of STAT3, leading to inhibition of the tyrosine phosphorylation, dimerization, nuclear translocation, and transcriptional activity of STAT3. The inhibitory effect of ODZ10117 on STAT3 was stronger than the known STAT3 inhibitors such as S3I-201, STA-21, and nifuroxazide. ODZ10117 suppressed the migration and invasion, induced apoptosis, reduced tumor growth and lung metastasis, and extended the survival rate in both in vitro and in vivo models of breast cancer. Overall, we demonstrated that ODZ10117 is a novel STAT3 inhibitor and may be a promising agent for the development of anticancer drugs.

Indexed as

3-(2,4-Dichloro-phenoxymethyl)-5-trichloromethyl-[1,2,4]oxadiazole (ODZ10117)cell-based high-throughput screeningSH2 domainSTAT3structure-based computational database screeningtargeted therapy

Identifiers

PMID31684051
PMCPMC6912340
OpenAlexW2986540263

What OpenQuestion holds

Textmetadata
LicenceCC BY
Read underepoch 390

Registered trials

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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.