Evidence map›Paper›PMID 30689946›Full record

ArticleJournal of medicinal chemistry2019

2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action.

Benoît Bestgen, Irina Kufareva, Weiguang Seetoh, Chris Abell, Rolf W Hartmann, Ruben Abagyan, Marc Le Borgne, Odile Filhol, Claude Cochet, Thierry Lomberget and 1 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2019. 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
1.2field-weighted citation impact, top 22% 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, 27 citations in OpenAlex.

  1. Review
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  8. Development and therapeutic potential of 2-aminothiazole derivatives in anticancer drug discovery.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2021
    Review
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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

11 authors at 6 institutions in 4 countries.

Benoît BestgenUniversité de Lyon, Université Lyon 1, Faculté de Pharmacie, ISPB, EA 4446 Bioactive Molecules and Medicinal Chemistry, SFR Santé Lyon-Est CNRS UMS3453, INSERM US7, 69373 Lyon Cedex 8, France.ORCID 0000-0002-2019-2113
Irina KufarevaSkaggs School of Pharmacy and Pharmaceutical Sciences , University of California, San Diego , La Jolla , California 92093 , United States.ORCID 0000-0001-9083-7039
Weiguang SeetohDepartment of Chemistry , University of Cambridge , Lensfield Road , Cambridge CB2 1EW , U.K.ORCID 0000-0002-1138-6581
Chris AbellDepartment of Chemistry , University of Cambridge , Lensfield Road , Cambridge CB2 1EW , U.K.ORCID 0000-0001-9174-1987
Rolf W HartmannDepartment of Drug Design and Optimization , Helmholtz Institute for Pharmaceutical Research Saarland (HIPS) , Campus C2.3, 66123 Saarbrücken , Germany.ORCID 0000-0002-5871-5231
Ruben AbagyanSkaggs School of Pharmacy and Pharmaceutical Sciences , University of California, San Diego , La Jolla , California 92093 , United States.ORCID 0000-0001-9309-2976
Marc Le BorgneUniversité de Lyon, Université Lyon 1, Faculté de Pharmacie, ISPB, EA 4446 Bioactive Molecules and Medicinal Chemistry, SFR Santé Lyon-Est CNRS UMS3453, INSERM US7, 69373 Lyon Cedex 8, France.ORCID 0000-0003-1398-075X
Odile FilholInstitut National de la Santé et de la Recherche Médicale , U1036, 38000 Grenoble , France.ORCID 0000-0003-1964-7958
Claude CochetInstitut National de la Santé et de la Recherche Médicale , U1036, 38000 Grenoble , France.ORCID 0000-0002-1772-4270
Thierry LombergetUniversité de Lyon, Université Lyon 1, Faculté de Pharmacie, ISPB, EA 4446 Bioactive Molecules and Medicinal Chemistry, SFR Santé Lyon-Est CNRS UMS3453, INSERM US7, 69373 Lyon Cedex 8, France.ORCID 0000-0002-4071-0002
Matthias EngelPharmaceutical and Medicinal Chemistry , Saarland University , Campus C2.3, 66123 Saarbrücken , Germany.ORCID 0000-0001-5065-8634
Université Claude Bernard Lyon 1 · FRInserm · FRUniversity of California San Diego · USUniversity of Cambridge · GBHelmholtz Institute for Pharmaceutical Research Saarland · DESaarland University · DE

Funding

AIBP and regulation of neuropathic painR01NS102432 · NINDS · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI MILLER, YURY, YAKSH, TONY L. · 2017 to 2021
$3.0M
The structural plasticity of chemokine and gp120 recognition by CCR5R01AI118985 · NIAID · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI HANDEL, TRACY M, KUFAREVA, IRINA · 2015 to 2019
$2.7M
Chemokine interaction with CXCR4 and ACKR3: structure and activation mechanismsR01GM117424 · NIGMS · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI HANDEL, TRACY M, KUFAREVA, IRINA · 2016 to 2019
$2.2M
Novel Druggable Exosites in Protein KinasesR01GM074832 · NIGMS · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI ABAGYAN, RUBEN · 2006 to 2009
$1.4M
NIAID NIH HHS R01 AI118985NIGMS NIH HHS R01 GM074832NIGMS NIH HHS R01 GM117424
6 · The paper itself

Abstract

Protein CK2 has gained much interest as an anticancer drug target in the past decade. We had previously described the identification of a new allosteric site on the catalytic α-subunit, along with first small molecule ligands based on the 4-(4-phenylthiazol-2-ylamino)benzoic acid scaffold. In the present work, structure optimizations guided by a binding model led to the identification of the lead compound 2-hydroxy-4-((4-(naphthalen-2-yl)thiazol-2-yl)amino)benzoic acid (27), showing a submicromolar potency against purified CK2α (IC

Indexed as

Allosteric RegulationAllosteric SiteAntineoplastic AgentsApoptosisBenzoatesCasein Kinase IICell Line, TumorHumansLigandsMolecular Docking SimulationMolecular StructureNaphthyridinesPhenazinesProdrugsProtein BindingProtein Kinase InhibitorsAntineoplastic AgentsBenzoatesCasein Kinase IICSNK2A1 protein, humanLigandsNaphthyridinesPhenazinesProdrugsProtein Kinase InhibitorssilmitasertibThiazoles

Identifiers

PMID30689946
PMCPMC7579840
OpenAlexW2914663185

What OpenQuestion holds

Textmetadata
LicenceTDM
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.