Isolation and structure of chaetomellic acids A and B from Chaetomella acutiseta: farnesyl pyrophosphate mimic inhibitors of ras farnesyl-protein transferase
| Autor: | Ralph T. Mosley, Rosalind G. Jenkins, Jackson B. Gibbs, Suresh B. Singh, Gerald F. Bills, Mary Nallin-Omstead, Keith C. Silverman, Deborah L. Zink, Georg Albers-Schönberg, Russell B. Lingham, Michael A. Goetz, Jerrold M. Liesch |
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| Rok vydání: | 1993 |
| Předmět: |
chemistry.chemical_classification
Farnesyl Protein Transferase biology Stereochemistry Farnesyltransferase Organic Chemistry Farnesyl pyrophosphate Biological activity Biochemistry chemistry.chemical_compound Enzyme Dicarboxylic acid chemistry Enzyme inhibitor Drug Discovery biology.protein Transferase |
| Zdroj: | Tetrahedron. 49:5917-5926 |
| ISSN: | 0040-4020 |
| DOI: | 10.1016/s0040-4020(01)87178-7 |
| Popis: | Farnesyl-Protein transferase catalyses a post-translational modification of Ras that is obligatory for the cell transforming activity of this oncogene protein. The screening of natural products to identify inhibitors of this enzyme as a potential anticancer agents, has led to the isolation of two novel dicarboxylic acids, named chaetomellic acids from Chaetomella acutiseta, as potent and selective inhibitors which appear to be the first examples of nonphosphorous containing FPP mimics. |
| Databáze: | OpenAIRE |
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