Generation of the UFM1 Toolkit for Profiling UFM1-Specific Proteases and Ligases.
Angew Chem Int Ed Engl
; 57(43): 14164-14168, 2018 10 22.
Article
em En
| MEDLINE
| ID: mdl-30188611
ABSTRACT
Ubiquitin-fold modifierâ
1 (UFM1) is a reversible post-translational modifier that is covalently attached to target proteins through an enzymatic cascade and removed by designated proteases. Abnormalities in this process, referred to as Ufmylation, have been associated with a variety of human diseases. Given this, the UFM1-specific enzymes represent potential therapeutic targets; however, understanding of their biological function has been hampered by the lack of chemical tools for activity profiling. To address this unmet need, a diversifiable platform for UFM1 activity-based probes (ABPs) utilizing a native chemical ligation (NCL) strategy was developed, enabling the generation of a variety of tools to profile both UFM1 conjugating and deconjugating enzymes. The use of the probes is demonstrated inâ
vitro and inâ
vivo for monitoring UFM1 enzyme reactivity, opening new research avenues.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Peptídeo Hidrolases
/
Sondas Moleculares
/
Proteínas
/
Processamento de Proteína Pós-Traducional
Limite:
Humans
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article