Glycosynthase variants for glycoprotein engineering and methods of use
US11203645B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jun 27, 2019 |
| Grant date | Dec 21, 2021 |
| Priority date | — |
| Expiry date | Jun 27, 2039 |
Classification
- Technology area (CPC G)Physics
- CPC primaryG01N2030/386
- WIPO fieldMeasurement
- WIPO sectorInstruments
Abstract
The present disclosure relates to novel glycosynthase enzymes for glycoprotein engineering and/or homogeneous antibody remodeling. The enzyme variants, termed EndoSd-D232M and EndoSz-D234M, contain the glycan conjugation and/or modification activity at the conserved N297 glycosylation site of Fc region of an exemplary antibody. It has been demonstrated that the glycosynthase activities of EndoSd-D232M and EndoSz-D234M can be applied to various mAbs targeting different receptors, including, but not limited to, Globo H, SSEA-4, SSEA-3 series of receptors (OBI-888; Globo H ganglioside), Herceptin (Her 2 receptor), Perj eta (Her 2 receptor) and Vectibix (EGFR receptor). It has been found that both mAb-GlcNAc and mAb-GlucNAc(F) were suitable substrates for both EndoSd-D232M and EndoSz-D234M. The ADCC assay of related products, OBI-888-G2S2 and Herceptin-G2S2, showed that the remodeled homogeneous antibody, mAb-G2S2, has an increased relative activity ranging from 3 to 26 folds.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.