N-substituted sultam carboxylic acids as novel glycogen synthase activators
| Autor: | Kuo-Sen Huang, Joseph A. Sergi, Stuart Hayden, Yonglin Ren, Weiya Yun, Qing Xiang, Mei Liu, Andrée R. Olivier, Yimin Qian, Karin Conde-Knape, Lin Yi, Xiaolei Zhang, David Robert Bolin, Paul Gillespie |
|---|---|
| Rok vydání: | 2013 |
| Předmět: |
Pharmacology
chemistry.chemical_classification biology Glycogen Organic Chemistry Pharmaceutical Science Skeletal muscle Biochemistry Glycogen debranching enzyme chemistry.chemical_compound Glycogen phosphorylase Enzyme medicine.anatomical_structure chemistry Drug Discovery Glycogen branching enzyme biology.protein medicine Molecular Medicine Glycogen synthase Phosphorylase kinase |
| Zdroj: | MedChemComm. 4:833-838 |
| ISSN: | 2040-2511 2040-2503 |
| Popis: | Decreased glycogen synthesis and turnover is a common defect in type 2 diabetic patients. Activating glycogen synthase, the enzyme that catalyses the transfer of glucose from UDP-glucose to a glycogen polymer chain, could be a potential therapeutic target for the treatment of diabetes. We discovered a series of N-substituted sultam carboxylic acids as potent glycogen synthase activators. Treatment of human skeletal muscle cells with these compounds resulted in an increase in glycogen synthesis. Compound 4 displayed good oral bioavailability and therefore may be a useful tool molecule to study GS as a potential anti-diabetic target. |
| Databáze: | OpenAIRE |
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