Structure-based design of caspase-1 inhibitor containing a diphenyl ether sulfonamide
| Autor: | John R. Rubin, Nigel Walker, Kenneth Dale Brady, Winnie W. Wong, Mark S. Plummer, Christine Humblet, Charles J. Stankovic, Aurash B Shahripour, Connolly Michael Kevin, Robert V. Talanian, Elizabeth A. Lunney, Hamish Allen, Tomi K. Sawyer |
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| Rok vydání: | 2001 |
| Předmět: |
Models
Molecular Stereochemistry Clinical Biochemistry Pharmaceutical Science Ether Crystal structure Biochemistry Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Enzyme Inhibitors Molecular Biology chemistry.chemical_classification Sulfonamides biology Caspase 1 Organic Chemistry Diphenyl ether Active site Caspase Inhibitors Combinatorial chemistry Sulfonamide Enzyme chemistry Enzyme inhibitor Drug Design biology.protein Molecular Medicine Ethers |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 11:2779-2782 |
| ISSN: | 0960-894X |
| Popis: | A series of compounds was designed and prepared as inhibitors of interleukin-1β converting enzyme (ICE), also known as caspase-1. These inhibitors, which employ a diphenyl ether sulfonamide, were designed to improve potency by forming favorable interactions between the diphenyl ether rings and the prime side hydrophobic region. An X-ray crystal structure of a representative member of the diphenyl ether sulfonamide series bound to the active site of caspase-1 was obtained. |
| Databáze: | OpenAIRE |
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