The squalestatins: potent inhibitors of squalene synthase. The role of the tricarboxylic acid moiety
| Autor: | Nigel S. Watson, B. E. Kirk, Ian P. Steeples, Richard Bell, Chuen Chan, Julia Widdowson, Julie L. Hutson, Brian Cox, Keeling Suzanne Elaine, Panayiotis A. Procopiou |
|---|---|
| Rok vydání: | 1993 |
| Předmět: |
chemistry.chemical_classification
ATP synthase biology Stereochemistry Organic Chemistry Clinical Biochemistry Pharmaceutical Science Tricarboxylic acid Inhibitory postsynaptic potential Biochemistry In vitro Squalene chemistry.chemical_compound Enzyme chemistry Enzyme inhibitor Drug Discovery biology.protein Molecular Medicine Moiety Molecular Biology |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 3:2541-2546 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(01)80713-7 |
| Popis: | In squalestatins possessing at C6 either a 4,6-dimethyloctenoate ester or a hydroxyl group, the 5-carboxylic acid is crucial for squalene synthase inhibitory activity. In the former seires, free carboxylic acids are not required at C3 or C4 for potent enzyme inhibitory activity whereas in the latter series esterification of the carboxylic acids at C3 or C4 results in a significant reduction in enzyme inhibitory activity. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|