biostudies-literatureKurhade SENational Institute of General Medical SciencesNIGMS NIH HHS12313-12318https://www.ebi.ac.uk/biostudies/studies/S-EPMC8131250biostudies-literatureUnknown60(22)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 construAngewandte Chemie (International ed. in English)Functionalized High Mannose-Specific Lectins for the Discovery of Type I Mannosidase Inhibitors.PMC8131250P20 GM113117GM113117P20 GM103638GM110761P50 GM069663P30 GM110761Gao FPWeiner JDFarrell MPKurhade SEfalseFunctionalized High Mannose-Specific Lectins for the Discovery of Type I Mannosidase Inhibitors.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 constru2021-01-01T00:00:00Z2021 May2026-05-31T09:48:52.071Z2025-02-18T23:32:22.023ZS-EPMC81312503372878710.1002/anie.202101249