Evidence map›Paper›PMID 35675124›Full record

ArticleACS chemical biology2022

Sialic Acid Derivatives Inhibit SiaT Transporters and Delay Bacterial Growth.

Tiago Bozzola, Mariafrancesca Scalise, Christer U Larsson, Michael C Newton-Vesty, Caterina Rovegno, Ankita Mitra, Jonathan Cramer, Weixiao Yuan Wahlgren, Partha Radhakrishnan Santhakumari, Richard E Johnsson and 8 more

Open access · hybridAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in ACS chemical biology, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing 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

5 citing papers in PubMed, 17 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

18 authors at 10 institutions in 7 countries.

Tiago BozzolaCentre for Analysis and Synthesis, Department of Chemistry, Lund University, P.O. Box 124, SE-221 00 Lund, Sweden.
Mariafrancesca ScaliseDepartment DiBEST (Biologia, Ecologia, Scienze della Terra) Unit of Biochemistry and Molecular Biotechnology, University of Calabria, Via P. Bucci 4C, 87036 Arcavacata di Rende, Italy.
Christer U LarssonDivision of Applied Microbiology, Department of Chemistry, Lund University, 22100 Lund, Sweden.
Michael C Newton-VestyBiomolecular Interaction Centre and School of Biological Sciences, University of Canterbury, 8140 Christchurch, New Zealand.
Caterina RovegnoCentre for Analysis and Synthesis, Department of Chemistry, Lund University, P.O. Box 124, SE-221 00 Lund, Sweden.
Ankita MitraCentre for Analysis and Synthesis, Department of Chemistry, Lund University, P.O. Box 124, SE-221 00 Lund, Sweden.
Jonathan CramerMolecular Pharmacy Group, Department of Pharmaceutical Sciences, University of Basel, Klingelbergstrasse 50, 4056 Basel, Switzerland.ORCID 0000-0001-9869-5645
Weixiao Yuan WahlgrenDepartment of Chemistry and Molecular Biology, University of Gothenburg, Box 462, S-40530 Gothenburg, Sweden.
Partha Radhakrishnan SanthakumariInstitute for Stem Cell Science and Regenerative Medicine, Bengaluru, Karnataka 560065, India.
Richard E JohnssonRed Glead Discovery AB, Medicon Village, 223 81 Lund, Sweden.
Oliver SchwardtMolecular Pharmacy Group, Department of Pharmaceutical Sciences, University of Basel, Klingelbergstrasse 50, 4056 Basel, Switzerland.
Beat ErnstMolecular Pharmacy Group, Department of Pharmaceutical Sciences, University of Basel, Klingelbergstrasse 50, 4056 Basel, Switzerland.ORCID 0000-0001-5787-2297
Rosmarie FriemannDepartment of Clinical Microbiology, Sahlgrenska University Hospital, 41345 Gothenburg, Sweden.
Renwick C J DobsonBiomolecular Interaction Centre and School of Biological Sciences, University of Canterbury, 8140 Christchurch, New Zealand.
Cesare IndiveriDepartment DiBEST (Biologia, Ecologia, Scienze della Terra) Unit of Biochemistry and Molecular Biotechnology, University of Calabria, Via P. Bucci 4C, 87036 Arcavacata di Rende, Italy.ORCID 0000-0001-9818-6621
Jenny SchelinDivision of Applied Microbiology, Department of Chemistry, Lund University, 22100 Lund, Sweden.
Ulf J NilssonCentre for Analysis and Synthesis, Department of Chemistry, Lund University, P.O. Box 124, SE-221 00 Lund, Sweden.ORCID 0000-0001-5815-9522
Ulf EllervikCentre for Analysis and Synthesis, Department of Chemistry, Lund University, P.O. Box 124, SE-221 00 Lund, Sweden.ORCID 0000-0001-5287-0137
Lund University · SEUniversity of Basel · CHInstitute of Biomembranes, Bioenergetics and Molecular Biotechnologies · ITManipal Academy of Higher Education · INMedicon Village · SESahlgrenska University Hospital · SEThe University of Melbourne · AUUniversity of Calabria · ITUniversity of Canterbury · NZUniversity of Gothenburg · SE

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Antibiotic resistance is a major worldwide concern, and new drugs with mechanistically novel modes of action are urgently needed. Here, we report the structure-based drug design, synthesis, and evaluation in vitro and in cellular systems of sialic acid derivatives able to inhibit the bacterial sialic acid symporter SiaT. We designed and synthesized 21 sialic acid derivatives and screened their affinity for SiaT by a thermal shift assay and elucidated the inhibitory mechanism through binding thermodynamics, computational methods, and inhibitory kinetic studies. The most potent compounds, which have a 180-fold higher affinity compared to the natural substrate, were tested in bacterial growth assays and indicate bacterial growth delay in methicillin-resistant

Indexed as

Methicillin-Resistant Staphylococcus aureusAnti-Bacterial AgentsKineticsMicrobial Sensitivity TestsN-Acetylneuraminic AcidAnti-Bacterial AgentsN-Acetylneuraminic Acid

Identifiers

PMID35675124
PMCPMC9295122
OpenAlexW4281667029

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.