Furan warheads for covalent trapping of weak protein-protein interactions: cross-linking of thymosin ß4 to actin.
Chem Commun (Camb)
; 57(49): 6054-6057, 2021 Jun 21.
Article
em En
| MEDLINE
| ID: mdl-34036992
ABSTRACT
We describe furan as a triggerable 'warhead' for site-specific cross-linking using the actin and thymosin ß4 (Tß4)-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' Tß4-variants provides initial proof to further exploit furan-technology for covalent drug design targeting lysines.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Idioma:
En
Ano de publicação:
2021
Tipo de documento:
Article