Substrate Analog-based N-Glycosylation Inhibitor Development Service at CD BioGlyco

CD BioGlyco is experienced in Glycosylation Inhibitor development. N-Glycosylation is a co-translational or post-translational modification of nascent peptide chains. N-Glycosylation is found to play a crucial role in biological growth, etc. A variety of diseases are associated with N-glycosylation abnormalities. The development of N-Glycosylation Inhibitors is important for studying their function and disease treatment methods. Substrate analog inhibitors affect substrate-enzyme binding by competing with the substrate for the enzyme binding site. Based on published synthetic methods for inhibitors and our extensive experience in glycosylation research, we offer substrate analog-based N-glycosylation inhibitor development services. We focus our research on the direction of acceptor analogs, donor analogs, and dual-substrate inhibitors of N-glycosylation-related enzymes.

• Donor analog inhibitor development service

Donor-analog inhibitors bind to the active center of an enzyme and occupy the binding site of the natural donor to achieve competitive inhibition. We are skilled in high-throughput screening techniques and screen tens of thousands of compounds on a large scale.

• Receptor analog inhibitor development service

Receptor analogs are another type of substrate analog. Since N-glycosylation-related enzymes exhibit strict selectivity for receptor substrates. Therefore, the development of inhibitors based on receptor substrates may address this issue of selectivity. We try to screen and synthesize inhibitors with strong inhibitory effects and high selectivity to achieve precise regulation of N-glycosylation.

• Dual-substrate inhibitor development service

The natural donor substrate binds to the enzyme more than the natural acceptor substrate. The selectivity of the enzyme, however, is only related to the acceptor substrate. To develop inhibitors with high binding force and high selectivity, we screen and synthesize dual-substrate inhibitors and study their inhibitory effects.

Fig.1 Direction of N-glycosylation inhibitor development based on substrate analogs. (CD BioGlyco)

Publication

Technology: Synthesis of bioconjugates

Journal: European Journal of Pharmaceutical Sciences

IF: 4.6

Published: 2022

Results: 18β-Glycyrrhetinic acid (18β-GA) possesses several biological activities. In this study, the in vitro antiglycation and α-glucosidase inhibitory activities of several 18β-GA -peptide conjugates were evaluated. The results revealed that an 18β-GA -peptide conjugate 5 (compound 5) was an α-glucosidase competitive inhibitor. It competitively binds to the active site residues of the enzyme with the substrate, thus inhibiting the enzyme activity. It was found to be non-cytotoxic by assay and is a highly effective competitive inhibitor.

Fig.2 Mode of inhibition of α-glucosidase by compound 5. (Khan, et al., 2022)

Applications

• N-Glycosylation plays a role in many processes that affect disease progression. The development of N-glycosylation inhibitors plays a role in the research of disease pathogenesis.
• Protein N-glycosylation modifications play an important role in plant growth and development. N-Glycosylation inhibitors can affect N-glycosylation modifications, which in turn affect plant development.
• The development of N-glycosylation inhibitors has an important role in the research of therapeutic approaches for diabetes and other diseases.

Highlights of Us

• We have high throughput screening capability to screen tens of thousands of compounds on a scale.
• We have sufficient screening resources to provide a wide range of screened compound libraries and inhibitors.
• Differences in the modification of protein N-glycosylation in vivo at different stages of development can lead to differences in certain types of glycoforms. The development of inhibitors of N-glycosylation helps to study differences in the modification of N-glycosylation.

CD BioGlyco is dedicated to the discovery of highly potent and specific N-glycosylation inhibitors. We aim to contribute to the discovery and research of potentially novel preventive, therapeutic drugs, etc. In addition to N-glycosylation inhibitors, we also provide O-Glycosylation Inhibitor development services, etc. Please feel free to contact us for more detailed N-glycosylation inhibitor development programs and specific experimental procedures.