Evidence map›Paper›PMID 27775243›Full record

ArticleChemMedChem2016

Design and Synthesis of Fluorescent Acyclic Nucleoside Phosphonates as Potent Inhibitors of Bacterial Adenylate Cyclases.

Petra Břehová, Markéta Šmídková, Jan Skácel, Martin Dračínský, Helena Mertlíková-Kaiserová, Monica P Soto Velasquez, Val J Watts, Zlatko Janeba

Open access · greenAbstract read
In one paragraph

Article in ChemMedChem, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
1.5field-weighted citation impact, top 17% 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

6 citing papers in PubMed, 11 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

8 authors at 2 institutions in 2 countries.

Petra BřehováThe Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, Flemingovo nám. 2, 166 10, Prague 6, Czech Republic.
Markéta ŠmídkováThe Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, Flemingovo nám. 2, 166 10, Prague 6, Czech Republic.
Jan SkácelThe Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, Flemingovo nám. 2, 166 10, Prague 6, Czech Republic.
Martin DračínskýThe Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, Flemingovo nám. 2, 166 10, Prague 6, Czech Republic.
Helena Mertlíková-KaiserováThe Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, Flemingovo nám. 2, 166 10, Prague 6, Czech Republic.
Monica P Soto VelasquezDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN, 47907, USA.
Val J WattsDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN, 47907, USA.
Zlatko JanebaThe Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, Flemingovo nám. 2, 166 10, Prague 6, Czech Republic.ORCID 0000-0003-4654-679X
Czech Academy of Sciences, Institute of Organic Chemistry and Biochemistry · CZPurdue University West Lafayette · US

Funding

Understanding adaptive signaling of neuronal adenyly cyclases using siRNAR33MH101673 · NIMH · PURDUE UNIVERSITY · PI WATTS, VAL J · 2015 to 2016
$889k
Understanding adaptive signaling of neuronal adenyly cyclases using siRNAR21MH101673 · NIMH · PURDUE UNIVERSITY · PI WATTS, VAL J · 2014 to 2014
$261k
NIMH NIH HHS R21 MH101673NIMH NIH HHS R33 MH101673
6 · The paper itself

Abstract

Bordetella pertussis adenylate cyclase toxin (ACT) and Bacillus anthracis edema factor (EF) are key virulence factors with adenylate cyclase (AC) activity that substantially contribute to the pathogenesis of whooping cough and anthrax, respectively. There is an urgent need to develop potent and selective inhibitors of bacterial ACs with prospects for the development of potential antibacterial therapeutics and to study their molecular interactions with the target enzymes. Novel fluorescent 5-chloroanthraniloyl-substituted acyclic nucleoside phosphonates (Cl-ANT-ANPs) were designed and synthesized in the form of their diphosphates (Cl-ANT-ANPpp) as competitive ACT and EF inhibitors with sub-micromolar potency (IC

Indexed as

Drug DesignAdenylyl Cyclase InhibitorsAdenylyl CyclasesAnimalsBordetella pertussisDose-Response Relationship, DrugFluorescent DyesMacrophagesMiceMolecular StructureNucleosidesOrganophosphonatesStructure-Activity RelationshipAdenylyl Cyclase InhibitorsAdenylyl CyclasesFluorescent DyesNucleosidesOrganophosphonatesadenylate cyclaseanthraxantibacterial agentsfluorescencewhooping cough

Identifiers

PMID27775243
PMCPMC5198786
OpenAlexW2537585745

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.