A Robust α-L-Fucosidase from Prevotella nigrescens for Glycoengineering Therapeutic AntibodiesShow others and affiliations
2024 (English)In: ACS Chemical Biology, ISSN 1554-8929, E-ISSN 1554-8937, Vol. 19, no 7, p. 1515-1524Article in journal (Refereed) Published
Abstract [en]
Eliminating the core fucose from the N-glycans of the Fc antibody segment by pathway engineering or enzymatic methods has been shown to enhance the potency of therapeutic antibodies, especially in the context of antibody-dependent cytotoxicity (ADCC). However, there is a significant challenge due to the limited defucosylation efficiency of commercially available α-l-fucosidases. In this study, we report a unique α-l-fucosidase (PnfucA) from the bacterium Prevotella nigrescens that has a low sequence identity compared with all other known α-l-fucosidases and is highly reactive toward a core disaccharide substrate with fucose α(1,3)-, α (1,4)-and α(1,6)-linked to GlcNAc, and is less reactive toward the Fuc-α(1,2)-Gal on the terminal trisaccharide of the oligosaccharide Globo H (Bb3). The kinetic properties of the enzyme, such as its Km and kcat, were determined and the optimized expression of PnfucA gave a yield exceeding 30 mg/L. The recombinant enzyme retained its full activity even after being incubated for 6 h at 37 °C. Moreover, it retained 92 and 87% of its activity after freezing and freeze-drying treatments, respectively, for over 28 days. In a representative glycoengineering of adalimumab (Humira), PnfucA showed remarkable hydrolytic efficiency in cleaving the α(1,6)-linked core fucose from FucGlcNAc on the antibody with a quantitative yield. This enabled the seamless incorporation of biantennary sialylglycans by Endo-S2 D184 M in a one-pot fashion to yield adalimumab in a homogeneous afucosylated glycoform with an improved binding affinity toward Fcγ receptor IIIa.
Place, publisher, year, edition, pages
2024. Vol. 19, no 7, p. 1515-1524
National Category
Biochemistry Molecular Biology Other Chemistry Topics
Identifiers
URN: urn:nbn:se:kth:diva-350832DOI: 10.1021/acschembio.4c00196ISI: 001253294400001OAI: oai:DiVA.org:kth-350832DiVA, id: diva2:1885093
Funder
The Swedish Foundation for International Cooperation in Research and Higher Education (STINT), KO2018-7936
Note
QC 20240722
2024-07-222024-07-222025-02-20Bibliographically approved