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  Non-carbohydrate glycomimetics as inhibitors of calcium(II)-binding lectins

Kuhaudomlarp, S., Siebs, E., Shanina, E., Topin, J., Joachim, I., da Silva Figueiredo Celestino Gomes, P., et al. (2021). Non-carbohydrate glycomimetics as inhibitors of calcium(II)-binding lectins. Angewandte Chemie International Edition, 60(15), 8104-8114. doi:10.1002/anie.202013217.

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 Creators:
Kuhaudomlarp, Sakonwan, Author
Siebs, Eike, Author
Shanina, Elena1, Author              
Topin, Jérémie, Author
Joachim, Ines, Author
da Silva Figueiredo Celestino Gomes, Priscila, Author
Varrot, Annabelle, Author
Rognan, Didier, Author
Rademacher, Christoph1, Author              
Imberty, Anne, Author
Titz, Alexander, Author
Affiliations:
1Christoph Rademacher, Biomolekulare Systeme, Max Planck Institute of Colloids and Interfaces, Max Planck Society, ou_1863300              

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Free keywords: carbohydrates, catechol, glycomimetic, lectin, PAINS
 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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Language(s): eng - English
 Dates: 2020-12-132021
 Publication Status: Published in print
 Pages: -
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Title: Angewandte Chemie International Edition
  Abbreviation : Angew. Chem., Int. Ed.
Source Genre: Journal
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Publ. Info: Weinheim : Wiley-VCH
Pages: - Volume / Issue: 60 (15) Sequence Number: - Start / End Page: 8104 - 8114 Identifier: ISSN: 1433-7851

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Title: Angewandte Chemie
  Abbreviation : Angew. Chem.
Source Genre: Journal
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Publ. Info: Weinheim : Wiley-VCH
Pages: - Volume / Issue: 133 (15) Sequence Number: - Start / End Page: 8185 - 8195 Identifier: ISSN: 0044-8249