Evidence map›Paper›PMID 33860211›Full record

ArticleACS pharmacology & translational science2021

Target-Driven Design of a Coumarinyl Chalcone Scaffold Based Novel EF2 Kinase Inhibitor Suppresses Breast Cancer Growth

Ferah Comert Onder, Nermin Kahraman, Esen Bellur Atici, Ali Cagir, Hakan Kandemir, Gizem Tatar, Tugba Taskin Tok, Goknur Kara, Bekir Karliga, Serdar Durdagi and 2 more

Erratum issuedOpen access · goldAbstract read
In one paragraph

Article in ACS pharmacology & translational science, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
1.3field-weighted citation impact, top 23% 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

7 citing papers in PubMed, 16 citations in OpenAlex.

  1. Article
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  6. Synthesis of Novel Triazine-Based Chalcones and 8,9-dihydro-7International journal of molecular sciences · 2024
    Article
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4 · The record

Corrections and comments

5 · Who and what money

Authors and funding

12 authors at 7 institutions in 2 countries.

Ferah Comert OnderDepartment of Experimental Therapeutics, The University of Texas, MD Anderson Cancer Center, 1515 Holcombe Boulevard, Unit 422, Houston, Texas 77030, United States.
Nermin KahramanDepartment of Experimental Therapeutics, The University of Texas, MD Anderson Cancer Center, 1515 Holcombe Boulevard, Unit 422, Houston, Texas 77030, United States.
Esen Bellur AticiDEVA Holding A.S. Cerkezkoy, 59500 Tekirdag, Turkey.
Ali CagirIzmir Institute of Technology, Department of Chemistry, Bioorganic and Medicinal Chemistry Laboratory, 35430 Urla, Turkey.
Hakan KandemirTekirdag Namik Kemal University, Department of Chemistry, 59030 Tekirdag, Turkey.
Gizem TatarGaziantep University, Institute of Health Sciences, Department of Bioinformatics and Computational Biology, 27310 Gaziantep, Turkey.
Tugba Taskin TokGaziantep University, Institute of Health Sciences, Department of Bioinformatics and Computational Biology, 27310 Gaziantep, Turkey.
Goknur KaraDepartment of Experimental Therapeutics, The University of Texas, MD Anderson Cancer Center, 1515 Holcombe Boulevard, Unit 422, Houston, Texas 77030, United States.
Bekir KarligaDEVA Holding A.S. Cerkezkoy, 59500 Tekirdag, Turkey.
Serdar DurdagiDepartment of Biophysics, School of Medicine, Computational Biology and Molecular Simulations Laboratory, Bahcesehir University, 34734 Istanbul, Turkey.
Mehmet AyDepartment of Chemistry, Natural Products and Drug Research Laboratory, Faculty of Science and Arts, Çanakkale Onsekiz Mart University, 17020 Canakkale, Turkey.
Bulent OzpolatDepartment of Experimental Therapeutics, The University of Texas, MD Anderson Cancer Center, 1515 Holcombe Boulevard, Unit 422, Houston, Texas 77030, United States.
The University of Texas MD Anderson Cancer Center · USÇanakkale Onsekiz Mart Üniversitesi · TRGaziantep University · TRSetas (Turkey) · TRBahçeşehir University · TRIzmir Institute of Technology · TRTekirdağ Namık Kemal University · TR

Funding

Novel Targeted Therapeutics for Breast CancerR01CA244344 · NCI · UNIVERSITY OF TX MD ANDERSON CAN CTR · PI OZPOLAT, BULENT · 2020 to 2024
$1.8M
NCI NIH HHS R01 CA244344
6 · The paper itself

Abstract

Eukaryotic elongation factor 2 kinase (eEF-2K) is an unusual alpha kinase involved in protein synthesis through phosphorylation of elongation factor 2 (EF2). eEF-2K is highly overexpressed in breast cancer, and its activity is associated with significantly shortened patient survival and proven to be a potential molecular target in breast cancer. The crystal structure of eEF-2K remains unknown, and there is no potent, safe, and effective inhibitor available for clinical applications. We designed and synthesized several generations of potential inhibitors. The effect of the inhibitors at the binding pocket of eEF-2K was analyzed after developing a 3D target model by using a domain of another α-kinase called myosin heavy-chain kinase A (MHCKA) that closely resembles eEF-2K.

Identifiers

PMID33860211
PMCPMC8033782
OpenAlexW3140709271

What OpenQuestion holds

Textmetadata
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.