Furan warheads for covalent trapping of weak protein-protein interactions : cross-linking of thymosin β4 to actin
- Author
- Laia Miret Casals (UGent) , Willem Vannecke (UGent) , Kurt Hoogewijs (UGent) , Gianluca Arauz-Garofalo, Marina Gay, Mireia Diaz-Lobo, Marta Vilaseca, Christophe Ampe (UGent) , Marleen Van Troys (UGent) and Annemieke Madder (UGent)
- Organization
- Abstract
- We describe furan as a triggerable 'warhead' for site-specific cross-linking using the actin and thymosin beta 4 (T beta 4)-complex as model of a weak and dynamic protein-protein interaction (PPI) with known 3D structure and with application potential in disease contexts. The identified cross-linked residues demonstrate that lysine is a target for the furan warhead. The presented in vitro validation of covalently acting 'furan-armed' T beta 4-variants provides initial proof to further exploit furan-technology for covalent drug design targeting lysines.
- Keywords
- CYSTIC-FIBROSIS SPUTUM, STRUCTURAL BASIS, OXYGEN, SITE, OXIDATION, ACID
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Citation
Please use this url to cite or link to this publication: http://hdl.handle.net/1854/LU-8721581
- MLA
- Miret Casals, Laia, et al. “Furan Warheads for Covalent Trapping of Weak Protein-Protein Interactions : Cross-Linking of Thymosin Β4 to Actin.” CHEMICAL COMMUNICATIONS, vol. 57, no. 49, 2021, pp. 6054–57, doi:10.1039/d1cc01731d.
- APA
- Miret Casals, L., Vannecke, W., Hoogewijs, K., Arauz-Garofalo, G., Gay, M., Diaz-Lobo, M., … Madder, A. (2021). Furan warheads for covalent trapping of weak protein-protein interactions : cross-linking of thymosin β4 to actin. CHEMICAL COMMUNICATIONS, 57(49), 6054–6057. https://doi.org/10.1039/d1cc01731d
- Chicago author-date
- Miret Casals, Laia, Willem Vannecke, Kurt Hoogewijs, Gianluca Arauz-Garofalo, Marina Gay, Mireia Diaz-Lobo, Marta Vilaseca, Christophe Ampe, Marleen Van Troys, and Annemieke Madder. 2021. “Furan Warheads for Covalent Trapping of Weak Protein-Protein Interactions : Cross-Linking of Thymosin Β4 to Actin.” CHEMICAL COMMUNICATIONS 57 (49): 6054–57. https://doi.org/10.1039/d1cc01731d.
- Chicago author-date (all authors)
- Miret Casals, Laia, Willem Vannecke, Kurt Hoogewijs, Gianluca Arauz-Garofalo, Marina Gay, Mireia Diaz-Lobo, Marta Vilaseca, Christophe Ampe, Marleen Van Troys, and Annemieke Madder. 2021. “Furan Warheads for Covalent Trapping of Weak Protein-Protein Interactions : Cross-Linking of Thymosin Β4 to Actin.” CHEMICAL COMMUNICATIONS 57 (49): 6054–6057. doi:10.1039/d1cc01731d.
- Vancouver
- 1.Miret Casals L, Vannecke W, Hoogewijs K, Arauz-Garofalo G, Gay M, Diaz-Lobo M, et al. Furan warheads for covalent trapping of weak protein-protein interactions : cross-linking of thymosin β4 to actin. CHEMICAL COMMUNICATIONS. 2021;57(49):6054–7.
- IEEE
- [1]L. Miret Casals et al., “Furan warheads for covalent trapping of weak protein-protein interactions : cross-linking of thymosin β4 to actin,” CHEMICAL COMMUNICATIONS, vol. 57, no. 49, pp. 6054–6057, 2021.
@article{8721581,
abstract = {{We describe furan as a triggerable 'warhead' for site-specific cross-linking using the actin and thymosin beta 4 (T beta 4)-complex as model of a weak and dynamic protein-protein interaction (PPI) with known 3D structure and with application potential in disease contexts. The identified cross-linked residues demonstrate that lysine is a target for the furan warhead. The presented in vitro validation of covalently acting 'furan-armed' T beta 4-variants provides initial proof to further exploit furan-technology for covalent drug design targeting lysines.}},
author = {{Miret Casals, Laia and Vannecke, Willem and Hoogewijs, Kurt and Arauz-Garofalo, Gianluca and Gay, Marina and Diaz-Lobo, Mireia and Vilaseca, Marta and Ampe, Christophe and Van Troys, Marleen and Madder, Annemieke}},
issn = {{1359-7345}},
journal = {{CHEMICAL COMMUNICATIONS}},
keywords = {{CYSTIC-FIBROSIS SPUTUM,STRUCTURAL BASIS,OXYGEN,SITE,OXIDATION,ACID}},
language = {{eng}},
number = {{49}},
pages = {{6054--6057}},
title = {{Furan warheads for covalent trapping of weak protein-protein interactions : cross-linking of thymosin β4 to actin}},
url = {{http://doi.org/10.1039/d1cc01731d}},
volume = {{57}},
year = {{2021}},
}
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