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  19F NMR-Guided Design of Glycomimetic Langerin Ligands

Wamhoff, E.-C., Hanske, J., Schnirch, L., Aretz, J., Grube, M., Varón Silva, D., et al. (2016). 19F NMR-Guided Design of Glycomimetic Langerin Ligands. ACS Chemical Biology, 11(9), 2407-2413. doi:10.1021/acschembio.6b00561.

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Item Permalink: http://hdl.handle.net/11858/00-001M-0000-002B-7EA5-1 Version Permalink: http://hdl.handle.net/11858/00-001M-0000-002B-BE85-4
Genre: Journal Article
Alternative Title : ACS Chemical Biology

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Wamhoff, Eike-Christian1, Author              
Hanske, Jonas1, Author              
Schnirch, Lennart, Author
Aretz, Jonas1, Author              
Grube, Maurice2, Author              
Varón Silva, Daniel3, Author              
Rademacher, Christoph1, Author              
Affiliations:
1Christoph Rademacher, Biomolekulare Systeme, Max Planck Institute of Colloids and Interfaces, Max Planck Society, ou_1863300              
2Daniel Varon-Silva, Biomolekulare Systeme, Max Planck Institute of Colloids and Interfaces, Max Planck Society, ou_1863302              
3Daniel Varón Silva, Biomolekulare Systeme, Max Planck Institute of Colloids and Interfaces, Max Planck Society, ou_1863302              

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 Abstract: C-type lectin receptors (CLRs) play a pivotal role in pathogen defense and immune homeostasis. Langerin, a CLR predominantly expressed on Langerhans cells, represents a potential target receptor for the development of anti-infectives or immunomodulatory therapies. As mammalian carbohydrate binding sites typically display high solvent exposure and hydrophilicity, the recognition of natural monosaccharide ligands is characterized by low affinities. Consequently, glycomimetic ligand design poses challenges that extend to the development of suitable assays. Here, we report the first application of 19F R2-filtered NMR to address these challenges for a CLR, i.e., Langerin. The homogeneous, monovalent assay was essential to evaluating the in silico design of 2-deoxy-2-carboxamido-α-mannoside analogs and enabled the implementation of a fragment screening against the carbohydrate binding site. With the identification of both potent monosaccharide analogs and fragment hits, this study represents an important advancement toward the design of glycomimetic Langerin ligands and highlights the importance of assay development for other CLRs.

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 Dates: 2016-07-262016-09-16
 Publication Status: Published in print
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 Identifiers: DOI: 10.1021/acschembio.6b00561
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Title: ACS Chemical Biology
Source Genre: Journal
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Publ. Info: Washington, D.C. : American Chemical Society
Pages: - Volume / Issue: 11 (9) Sequence Number: - Start / End Page: 2407 - 2413 Identifier: ISSN: 1554-8929