Evidence map›Paper›PMID 33314528›Full record

ArticleAngewandte Chemie (International ed. in English)2021

Non-Carbohydrate Glycomimetics as Inhibitors of Calcium(II)-Binding Lectins.

Sakonwan Kuhaudomlarp, Eike Siebs, Elena Shanina, Jérémie Topin, Ines Joachim, Priscila da Silva Figueiredo Celestino Gomes, Annabelle Varrot, Didier Rognan, Christoph Rademacher, Anne Imberty and 1 more

Open access · hybridAbstract read
In one paragraph

Article in Angewandte Chemie (International ed. in English), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.

0numbers the graph read from it
0cells of the map it votes in
15citing papers in PubMed
1.4field-weighted citation impact, top 18% 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

15 citing papers in PubMed, 24 citations in OpenAlex.

  1. Synthetic Ligands of Myeloid C-Type Lectin Receptors.Chembiochem : a European journal of chemical biology · 2026
    Review
  2. Article
  3. Article
  4. Review
  5. Article
  6. Review
  7. Lectin-Targeted Prodrugs Activated byJournal of medicinal chemistry · 2022
    Article
  8. Discovery ofJournal of medicinal chemistry · 2022
    Article
  9. Review
  10. Article
  11. Targeting the Central Pocket of the Pseudomonas aeruginosa Lectin LecA.Chembiochem : a European journal of chemical biology · 2022
    Article
  12. Review
  13. Article
  14. Non-Carbohydrate Glycomimetics as Inhibitors of Calcium(II)-Binding Lectins.Angewandte Chemie (International ed. in English) · 2021
    Article
  15. Article
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 3 institutions in 2 countries.

Sakonwan KuhaudomlarpUniversité Grenoble Alpes, CNRS, CERMAV, 38000, Grenoble, France.ORCID 0000-0003-4415-3781
Eike SiebsChemical Biology of Carbohydrates (CBCH), Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS), Helmholtz Centre for Infection Research, 66123, Saarbrücken, Germany.ORCID 0000-0002-7349-9872
Elena ShaninaDepartment of Biomolecular Systems, Max Planck Institute of Colloids and Interfaces, 14424, Potsdam, Germany.ORCID 0000-0003-4235-9452
Jérémie TopinUniversité Grenoble Alpes, CNRS, CERMAV, 38000, Grenoble, France.ORCID 0000-0003-1470-1206
Ines JoachimChemical Biology of Carbohydrates (CBCH), Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS), Helmholtz Centre for Infection Research, 66123, Saarbrücken, Germany.
Priscila da Silva Figueiredo Celestino GomesLaboratoire d'Innovation Thérapeutique, UMR 7200 CNRS-Université de Strasbourg, 67400, Illkirch, France.ORCID 0000-0001-7370-9596
Annabelle VarrotUniversité Grenoble Alpes, CNRS, CERMAV, 38000, Grenoble, France.ORCID 0000-0001-6667-8162
Didier RognanLaboratoire d'Innovation Thérapeutique, UMR 7200 CNRS-Université de Strasbourg, 67400, Illkirch, France.ORCID 0000-0002-0577-641X
Christoph RademacherDepartment of Biomolecular Systems, Max Planck Institute of Colloids and Interfaces, 14424, Potsdam, Germany.ORCID 0000-0001-7082-7239
Anne ImbertyUniversité Grenoble Alpes, CNRS, CERMAV, 38000, Grenoble, France.ORCID 0000-0001-6825-9527
Alexander TitzChemical Biology of Carbohydrates (CBCH), Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS), Helmholtz Centre for Infection Research, 66123, Saarbrücken, Germany.ORCID 0000-0001-7408-5084
Centre National de la Recherche Scientifique · FRGerman Center for Infection Research · DEMax Planck Society · DE

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Because of the antimicrobial resistance crisis, lectins are considered novel drug targets. Pseudomonas aeruginosa utilizes LecA and LecB in the infection process. Inhibition of both lectins with carbohydrate-derived molecules can reduce biofilm formation to restore antimicrobial susceptibility. Here, we focused on non-carbohydrate inhibitors for LecA to explore new avenues for lectin inhibition. From a screening cascade we obtained one experimentally confirmed hit, a catechol, belonging to the well-known PAINS compounds. Rigorous analyses validated electron-deficient catechols as millimolar LecA inhibitors. The first co-crystal structure of a non-carbohydrate inhibitor in complex with a bacterial lectin clearly demonstrates the catechol mimicking the binding of natural glycosides with LecA. Importantly, catechol 3 is the first non-carbohydrate lectin ligand that binds bacterial and mammalian calcium(II)-binding lectins, giving rise to this fundamentally new class of glycomimetics.

Indexed as

Adhesins, BacterialAnti-Bacterial AgentsCalciumCatecholsGlycosidesMicrobial Sensitivity TestsModels, MolecularMolecular StructurePseudomonas aeruginosaAdhesins, BacterialAnti-Bacterial AgentsCalciumcatecholCatecholsGlycosidesLecA protein, bacteriacarbohydratescatecholglycomimeticlectinPAINS

Identifiers

PMID33314528
PMCPMC8048816
OpenAlexW3111668370

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC
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.