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  Multivalent Ligands with Tailor‐Made Anion Binding Motif as Stabilizers of Protein–Protein Interactions

Bartsch, L., Bartel, M., Gigante, A., Iglesias‐Fernández, J., Ruiz-Blanco, Y. B., Beuck, C., et al. (2019). Multivalent Ligands with Tailor‐Made Anion Binding Motif as Stabilizers of Protein–Protein Interactions. Chembiochem, 20(13), 2921-2926. doi:10.1002/cbic.201900288.

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 Creators:
Bartsch, Lina1, Author
Bartel, Maria2, Author
Gigante, Alba1, Author
Iglesias‐Fernández, Javier3, Author              
Ruiz-Blanco, Yasser B.4, Author
Beuck, Christine5, Author
Briels, Jeroen2, Author
Toetsch, Niklas4, Author
Bayer, Peter5, Author
Sanchez-Garcia, Elsa3, 4, Author              
Ottmann, Christian1, 2, Author
Schmuck, Carsten1, Author
Affiliations:
1Department of Organic Chemistry, University of Duisburg-Essen, Universitätsstrasse 7, 45141 Essen, Germany, ou_persistent22              
2Department of Biomedical Engineering, Eindhoven University of Technology, P.O. Box 513, 5600 MB Eindhoven, The Netherlands, ou_persistent22              
3Research Group Sánchez-García, Max-Planck-Institut für Kohlenforschung, Max Planck Society, ou_1950289              
4Computational Biochemistry, Faculty of Biology, Center of Medical Biotechnology, University Duisburg-Essen, Universitätsstrasse 2, 45117 Essen, Germany, ou_persistent22              
5Structural and Medicinal Biochemistry, University of Duisburg-Essen, Universitätsstrasse 1-5, 45141 Essen, Germany, ou_persistent22              

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Free keywords: 14-3-3 proteins; C-Raf; guanidiniocarbonylpyrrol; protein-protein-interactions; stabilizers; Tau
 Abstract: Modulation of protein–protein interactions (PPIs) is essential for understanding and tuning biologically relevant processes. Although inhibitors for PPIs are widely used, the field still lacks the targeted design of stabilizers. Here, we report unnatural stabilizers based on the combination of multivalency effects and the artificial building block guanidiniocarbonylpyrrol (GCP), an arginine mimetic. Unlike other GCP‐based ligands that modulate PPIs in different protein targets, only a tetrameric design shows potent activity as stabilizer of the 14‐3‐3ζ/C‐Raf and 14‐3‐3ζ/Tau complexes in the low‐micromolar range. This evidences the role of multivalency for achieving higher specificity in the modulation of PPIs.

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Language(s): eng - English
 Dates: 2019-05-022019-06-062019-12-02
 Publication Status: Published online
 Pages: 6
 Publishing info: -
 Table of Contents: -
 Rev. Type: Peer
 Identifiers: DOI: 10.1002/cbic.201900288
 Degree: -

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Title: Chembiochem
  Other : Chembiochem
Source Genre: Journal
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Publ. Info: Weinheim, Germany : Wiley-VCH
Pages: - Volume / Issue: 20 (13) Sequence Number: - Start / End Page: 2921 - 2926 Identifier: ISSN: 1439-4227
CoNE: https://pure.mpg.de/cone/journals/resource/110978984568897