Furan warheads for covalent trapping of weak protein–protein interactions: cross-linking of thymosin β4 to actin-Reference-Cited by-同舟云学术

Furan warheads for covalent trapping of weak protein–protein interactions: cross-linking of thymosin β4 to actin

Published:2021 Issue:49 Volume:57 Page:6054-6057
ISSN:1359-7345
Container-title:Chemical Communications
language:en
Short-container-title:Chem. Commun.

Author:

Miret-Casals Laia¹²³⁴⁵^ORCID,Vannecke Willem¹²³⁴⁵,Hoogewijs Kurt¹²³⁴⁵^ORCID,Arauz-Garofalo Gianluca⁶⁷⁸⁹¹⁰^ORCID,Gay Marina⁶⁷⁸⁹¹⁰,Díaz-Lobo Mireia⁶⁷⁸⁹¹⁰,Vilaseca Marta⁶⁷⁸⁹¹⁰^ORCID,Ampe Christophe¹¹¹²⁴¹³¹⁴^ORCID,Van Troys Marleen¹¹¹²⁴¹³¹⁴^ORCID,Madder Annemieke¹²³⁴⁵^ORCID

Affiliation:

1. Organic and Biomimetic Chemistry Research Group

2. Department of Organic and Macromolecular Chemistry

3. Faculty of Science

4. Ghent University

5. Krijgslaan 281 S4

6. Institute for Research in Biomedicine (IRB Barcelona)

7. The Barcelona Institute of Science and Technology

8. Baldiri Reixac 10

9. Barcelona 08028

10. Spain

11. Department of Biomolecular Medicine

12. Faculty of Medicine and Health Sciences

13. Technologiepark 75

14. Ghent-Zwijnaarde B-9052

Abstract

Furan is used as a caged warhead to covalently target weak protein–protein interactions. Furan-thymosin β4 cross-links selectively and irreversibly with actin targeting lysine. Furan technology could be further exploited for covalent drug design.

Funder

Universiteit Gent

Fonds Wetenschappelijk Onderzoek

Publisher

Royal Society of Chemistry (RSC)

Subject

Materials Chemistry,Metals and Alloys,Surfaces, Coatings and Films,General Chemistry,Ceramics and Composites,Electronic, Optical and Magnetic Materials,Catalysis

Link

http://pubs.rsc.org/en/content/articlepdf/2021/CC/D1CC01731D

Reference28 articles.

1. Covalent inhibitors in drug discovery: from accidental discoveries to avoided liabilities and designed therapies

2. The resurgence of covalent drugs

3. New Electrophiles and Strategies for Mechanism-Based and Targeted Covalent Inhibitor Design

4. Sequence Specific DNA Cross-Linking Triggered by Visible Light

5. Singlet Oxygen-Induced Furan Oxidation for Site-Specific and Chemoselective Peptide Ligation

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