Projects Sharing Researchers
- Gerardus Boons
- Jun Guo
- Jinkeng Asong
|Project Title||Feedback Prodrugs|
Prodrugs are often used to minimize toxicity problems found with therapeutic compositions for a myriad of conditions. It has historically difficult to develop both drugs and prodrugs for inhibitors of glycosidases, which are involved in many vital cellular functions. Described herein is a feedback prodrug approach for glycosidase inhibitors which address many of the above issues.
University of Georgia researchers have developed a prodrug in the form of a conjugated compound that serves as a substrate for a lytic enzyme and includes, as a direct or indirect cleavage product, an inhibitor of that enzyme. Contact between the prodrug and the lytic enzyme releases the inhibitor and thereby inhibits the activity of the lytic enzyme through feedback inhibition.
The attraction of this approach is that the inhibitor will only be released at the site of the enzyme. Selectivity is achieved due to the specific selectivity of glycosidases for their substrates. Furthermore, only the amount of compound required for complete inhibition of the targeted enzyme is released. The remaining pool of prodrug will, however, be activated when active enzyme reappears thereby approximating conditions of continual infusion.
• Geert-Jan Boons, Distinguished Professor in Biochemical Sciences
• Jun Guo
• Jinkeng Asong
The research of the Boons Group deals with the synthesis and biological functions of carbohydrates and glycocongugates. The diversity of topics to which the group has significantly contributed include the development of new and better methods for synthesizing exceptionally complex molecules, the use of new methods in the synthesis and study of properties of complex carbohydrates of increasing size and complexity, the development of synthetic cancer and bacterial vaccines, the design and synthesis of glycosidase inhibitors and the use of synthetic compounds for the study of innate immunity
|Tags||Carbohydrate, Drug Manufacturing|
|Posted Date||Jul 5, 2017 10:38 AM|
|Patent Number||Issue Date||Type||Country of Filing|