ArticleAngewandte Chemie (International ed. in English)2021
Non-Carbohydrate Glycomimetics as Inhibitors of Calcium(II)-Binding Lectins.
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.
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Who cites it
15 citing papers in PubMed, 24 citations in OpenAlex.
- Synthetic Ligands of Myeloid C-Type Lectin Receptors.Chembiochem : a European journal of chemical biology · 2026Review
- The Parkinson's Disease Drug Tolcapone and Analogues are Potent Glycomimetic Lectin Inhibitors of Pseudomonas aeruginosa LecA.Angewandte Chemie (International ed. in English) · 2025Article
- Bispecific Thio-Linked Disaccharides as Inhibitors of Pseudomonas Aeruginosa Lectins LecA (PA-IL) and LecB (PA-IIL): Dual-Targeting Strategy.Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
- Glycomimetics for the inhibition and modulation of lectins.Chemical Society reviews · 2023Review
- Neutralizing the Impact of the Virulence Factor LecA from Pseudomonas aeruginosa on Human Cells with New Glycomimetic Inhibitors.Angewandte Chemie (International ed. in English) · 2023Article
- Involvement of sialoglycans in SARS-COV-2 infection: Opportunities and challenges for glyco-based inhibitors.IUBMB life · 2022Review
- Lectin-Targeted Prodrugs Activated byJournal of medicinal chemistry · 2022Article
- Discovery ofJournal of medicinal chemistry · 2022Article
- Structural Considerations for Building Synthetic Glycoconjugates as Inhibitors for Pseudomonas aeruginosa Lectins.ChemMedChem · 2022Review
- Targeting undruggable carbohydrate recognition sites through focused fragment library design.Communications chemistry · 2022Article
- Targeting the Central Pocket of the Pseudomonas aeruginosa Lectin LecA.Chembiochem : a European journal of chemical biology · 2022Article
- Medicinal chemistry of the myeloid C-type lectin receptors Mincle, Langerin, and DC-SIGN.RSC medicinal chemistry · 2021Review
- Pan-selectin inhibitors as potential therapeutics for COVID-19 treatment: in silico screening study.Glycobiology · 2021Article
- Non-Carbohydrate Glycomimetics as Inhibitors of Calcium(II)-Binding Lectins.Angewandte Chemie (International ed. in English) · 2021Article
- Discovering mycobacterial lectins as potential drug targets and vaccine candidates for tuberculosis treatment: a theoretical approach.Journal of proteins and proteomics · 2021Article
Corrections and comments
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Authors and funding
11 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
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.
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Registered trials
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.