Evidence map›Paper›PMID 32192199›Full record

ArticleInternational journal of molecular sciences2020

Benzothiazolyl Ureas are Low Micromolar and Uncompetitive Inhibitors of 17β-HSD10 with Implications to Alzheimer's Disease Treatment.

Monika Schmidt, Ondrej Benek, Lucie Vinklarova, Martina Hrabinova, Lucie Zemanova, Matej Chribek, Vendula Kralova, Lukas Hroch, Rafael Dolezal, Antonin Lycka and 6 more

Open access · goldAbstract read
In one paragraph

Article in International journal of molecular sciences, 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
1.2field-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

11 citing papers in PubMed, 21 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

16 authors at 5 institutions in 3 countries.

Monika SchmidtUniversity of Hradec Kralove, Faculty of Science, Department of Chemistry, Rokitanskeho 62, 500 03 Hradec Kralove, Czech Republic.ORCID 0000-0003-4984-9155
Ondrej BenekUniversity of Hradec Kralove, Faculty of Science, Department of Chemistry, Rokitanskeho 62, 500 03 Hradec Kralove, Czech Republic.ORCID 0000-0001-6840-1933
Lucie VinklarovaUniversity of Hradec Kralove, Faculty of Science, Department of Chemistry, Rokitanskeho 62, 500 03 Hradec Kralove, Czech Republic.
Martina HrabinovaUniversity Hospital Hradec Kralove, Biomedical Research Centre, Sokolska 581, 500 05 Hradec Kralove, Czech Republic.ORCID 0000-0002-9428-4109
Lucie ZemanovaUniversity of Hradec Kralove, Faculty of Science, Department of Chemistry, Rokitanskeho 62, 500 03 Hradec Kralove, Czech Republic.
Matej ChribekCharles University in Prague, Faculty of Pharmacy in Hradec Kralove, Department of Pharmaceutical Chemistry and Drug Control, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic.
Vendula KralovaCharles University in Prague, Faculty of Pharmacy in Hradec Kralove, Department of Pharmaceutical Chemistry and Drug Control, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic.
Lukas HrochUniversity Hospital Hradec Kralove, Biomedical Research Centre, Sokolska 581, 500 05 Hradec Kralove, Czech Republic.
Rafael DolezalUniversity of Hradec Kralove, Faculty of Science, Department of Chemistry, Rokitanskeho 62, 500 03 Hradec Kralove, Czech Republic.
Antonin LyckaUniversity of Hradec Kralove, Faculty of Science, Department of Chemistry, Rokitanskeho 62, 500 03 Hradec Kralove, Czech Republic.
Lukas PrchalUniversity Hospital Hradec Kralove, Biomedical Research Centre, Sokolska 581, 500 05 Hradec Kralove, Czech Republic.
Daniel JunUniversity of Defence, Faculty of Military Health Sciences, Department of Toxicology and Military Pharmacy, Trebesska 1575, 500 01 Hradec Kralove, Czech Republic.ORCID 0000-0002-0882-6304
Laura AitkenUniversity of St. Andrews, School of Biology, Medical and Biological Science Building, North Haugh, St. Andrews KY16 9TF, UK.ORCID 0000-0001-7259-4491
Frank Gunn-MooreUniversity of St. Andrews, School of Biology, Medical and Biological Science Building, North Haugh, St. Andrews KY16 9TF, UK.
Kamil KucaUniversity of Hradec Kralove, Faculty of Science, Department of Chemistry, Rokitanskeho 62, 500 03 Hradec Kralove, Czech Republic.ORCID 0000-0001-9664-1109
Kamil MusilekUniversity of Hradec Kralove, Faculty of Science, Department of Chemistry, Rokitanskeho 62, 500 03 Hradec Kralove, Czech Republic.ORCID 0000-0002-7504-4062
University Hospital Hradec Králové · CZUniversity of Hradec Králové · CZCharles University · CZUniversity of St Andrews · GBUniversity of Defence · RS

Funding

Ministerstvo Školství, Mládeže a Tělovýchovy CZ.02.1.01/0.0/0.0/18_069/0010054Ministerstvo Zdravotnictví Ceské Republiky NV19-09-00578NIMH NIH HHS no. ED2.1.00/03.0078University Hospital Hradec Kralove UHHK, 00179906University of Hradec Kralove Postdoctoral job positions at UHKUniversity of Hradec Kralove SV2115-2018University of Hradec Kralove VT2019-2021Wellcome Trust 204821/Z/16/Z
6 · The paper itself

Abstract

Human 17β-hydroxysteroid dehydrogenase type 10 is a multifunctional protein involved in many enzymatic and structural processes within mitochondria. This enzyme was suggested to be involved in several neurological diseases, e.g., mental retardation, Parkinson's disease, or Alzheimer's disease, in which it was shown to interact with the amyloid-beta peptide. We prepared approximately 60 new compounds based on a benzothiazolyl scaffold and evaluated their inhibitory ability and mechanism of action. The most potent inhibitors contained 3-chloro and 4-hydroxy substitution on the phenyl ring moiety, a small substituent at position 6 on the benzothiazole moiety, and the two moieties were connected via a urea linker (

Indexed as

3-Hydroxyacyl CoA DehydrogenasesAlzheimer DiseaseBenzothiazolesEnzyme ActivationEnzyme InhibitorsHumansKineticsMolecular StructureRecombinant ProteinsStructure-Activity RelationshipUrea3-Hydroxyacyl CoA DehydrogenasesBenzothiazolesEnzyme InhibitorsHSD17B10 protein, humanRecombinant ProteinsUrea17β-hydroxysteroid dehydrogenase type 10ABADAlzheimer’s diseasebenzothiazoleinhibitorneurodegeneration

Identifiers

PMID32192199
PMCPMC7139388
OpenAlexW3011373479

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.