Synthesis and biological activity of optimized belactosin C congeners
Copyright policy )Synthesis and biological activity of optimized belactosin C congeners
Successful biochemical studies of the natural products belactosin A and C as well as their more stable acylated derivatives have proved them to be powerful proteasome inhibitors and thereby potential candidates as pharmacologically relevant active compounds. In order to understand their structure-biological activity relations in detail and to find ways of improving their biological activity, four new modified belactosin congeners have been synthesized and tested. One of them (compound 6) turned out to be a more potent inhibitor against HeLa cells than the known proteasome inhibitor MG132.
- Center for Integrated Protein Science Munich Germany
- University of Göttingen Germany
- Technical University of Munich Germany
- Max Planck Society Germany
- Ludwig-Maximilians-Universität München Germany
Models, Molecular, Proteasome Endopeptidase Complex, Dose-Response Relationship, Drug, Molecular Structure, Leupeptins, Acylation, Blotting, Western, Antineoplastic Agents, Mice, Transgenic, Stereoisomerism, Cysteine Proteinase Inhibitors, Fibroblasts, Crystallography, X-Ray, Mice, Animals, Humans, Female, Peptides, Proteasome Inhibitors, HeLa Cells
Models, Molecular, Proteasome Endopeptidase Complex, Dose-Response Relationship, Drug, Molecular Structure, Leupeptins, Acylation, Blotting, Western, Antineoplastic Agents, Mice, Transgenic, Stereoisomerism, Cysteine Proteinase Inhibitors, Fibroblasts, Crystallography, X-Ray, Mice, Animals, Humans, Female, Peptides, Proteasome Inhibitors, HeLa Cells
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