Glycosylation inhibitors play an obvious role in the therapeutic research of diseases. CD BioGlyco has constructed an inhibitor development platform, which is dedicated to the Development of Glycosylation Inhibitors, and provides a wide range of inhibitor development services, such as O-N-acetylglucosamine (O-GlcNAc) transferase inhibitor development service.
Fig.1 Development content of O-GlcNAc transferase inhibitor. (CD BioGlyco)
Technology: Bundled in situ click chemistry
Journal: Journal of Medicinal Chemistry
Results: In this research, the authors utilized bundled in situ click chemistry (TISCC), using p-azidoiodoacetanilide as a bifunctional building block M. Sixty-one alkyne-based building blocks N were screened, and two cell-permeable O-GlcNAc transferase (OGT) inhibitors (APNT and APBT) were developed after subsequent chemical modifications. These two inhibitors were able to reduce O-GlcNAc glycosylation levels in cells without significant cytotoxicity. The unusual non-competitive inhibition for OGT contributes to the discovery of new inhibitors and the exploration of the regulatory mechanisms of OGT.
Fig.2 TISCC: (a) Screening of building blocks to discover the new candidate; (b) Synthesis of the new candidate for activity evaluation. (Wang, et al., 2016)
CD BioGlyco's glycosylation inhibitors are designed for specific research purposes or as a reference for a wide range of bioscience applications. We provide a wide range of glycosylation inhibitor development services and are always committed to serving researchers in different fields. At the same time, every program we develop is quality-tested to ensure client satisfaction. If you are interested in our services, please feel free to contact us.