Functionalized High Mannose-Specific Lectins for the Discovery of Typeâ
I Mannosidase Inhibitors.
Angew Chem Int Ed Engl
; 60(22): 12313-12318, 2021 05 25.
Article
em En
| MEDLINE
| ID: mdl-33728787
ABSTRACT
An engineered cyanovirin-N homologue that exhibits specificity for high mannose N-glycans has been constructed to aid typeâ
I α 1,2-mannosidase inhibitor discovery and development. Engineering the lectins C-terminus permitted facile functionalization with fluorophores via a sortase and click strategy. The resulting lectin constructs exhibit specificity for cells presenting high mannose N-glycans. Importantly, these lectin constructs can also be applied to specifically assess changes in cell surface glycosylation induced by typeâ
I mannosidase inhibitors. Testing the utility of these lectin constructs led to the discovery of typeâ
I mannosidase inhibitors with nanomolar potency. Cumulatively, these findings reveal the specificity and utility of the functionalized cyanovirin-N homologue constructs, and highlight their potential in analytical contexts that require high mannose-specific lectins.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Lectinas
/
Manosidases
Tipo de estudo:
Prognostic_studies
Limite:
Humans
Idioma:
En
Ano de publicação:
2021
Tipo de documento:
Article