Functionalized High Mannose-Specific Lectins for the Discovery of Type I Mannosidase Inhibitors.

ABSTRACT: An engineered cyanovirin-N homologue that exhibits specificity for high mannose N-glycans has been constructed to aid type 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 type I mannosidase inhibitors. Testing the utility of these lectin constructs led to the discovery of type I mannosidase inhibitors with nanomolar potency. Cumulatively, these findings reveal the specificity and utility of the functionalized cyanovirin-N homologue constru

SUBMITTER: Kurhade SE 

PROVIDER: S-EPMC8131250 | biostudies-literature | 2021 May

REPOSITORIES: biostudies-literature