Palau’amine and Related Oroidin Alkaloids Dibromophakellin and Dibromophakellstatin Inhibit the Human 20S Proteasome
| Autor: | Jetze J. Tepe, Shun Su, Ken S. Feldman, Amanda P. Skoumbourdis, Matthew D. Fodor, Ian B. Seiple, Theresa A. Lansdell, Nicole M. Hewlett, Phil S. Baran |
|---|---|
| Rok vydání: | 2012 |
| Předmět: |
Proteasome Endopeptidase Complex
Palau'amine Pharmaceutical Science Stereoisomerism Guanidines Heterocyclic Compounds 4 or More Rings 20s proteasome Article Analytical Chemistry chemistry.chemical_compound Alkaloids Drug Discovery Humans Cytotoxic T cell Pyrroles Spiro Compounds Pharmacology Microscopy Confocal Organic Chemistry Imidazoles NF-kappa B NFKB1 Dibromophakellstatin IκBα Complementary and alternative medicine Biochemistry chemistry Molecular Medicine Proteasome Inhibitors Dibromophakellin HeLa Cells |
| Zdroj: | Journal of Natural Products. 75:980-985 |
| ISSN: | 1520-6025 0163-3864 |
| Popis: | We report herein that the oroidin-derived alkaloids palau'amine (1), dibromophakellin (2), and dibromophakellstatin (3) inhibit the proteolytic activity of the human 20S proteasome as well as the (i)20S immunoproteasome catalytic core. Palau'amine is found to prevent the degradation of ubiquitinylated proteins, including IκBα, in cell culture, which may be indicative of the potential mechanism by which these agents exhibit their exciting cytotoxic and immunosuppressive properties. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|