Solution phase synthesis of a combinatorial library of chalcones and flavones as potent cathepsin V inhibitors
| Autor: | Paulo C. Vieira, Ariane Migliato Martinelli, Joel Alvim, Richele P. Severino, João B. Fernandes, Arlene G. Corrêa, Emerson F. Marques, M. Fátima das G. F. da Silva |
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| Rok vydání: | 2010 |
| Předmět: |
Cathepsin
chemistry.chemical_classification Molecular Structure Chemistry Stereochemistry T-Lymphocytes Proteolytic enzymes Stereoisomerism General Chemistry Cysteine Proteinase Inhibitors Flavones Cysteine protease Solution phase Cathepsins Solutions Cysteine Endopeptidases Structure-Activity Relationship Chalcones Cathepsin O Biochemistry Combinatorial Chemistry Techniques Humans Cathepsin V Solution phase synthesis |
| Zdroj: | Journal of combinatorial chemistry. 12(5) |
| ISSN: | 1520-4774 |
| Popis: | Cathepsin V is a papain-like cysteine protease. It is involved in the control of human T cells (responsible for cell immunity), and presents the largest elastolytic activity among the proteolytic enzymes. Therefore, cathepsin V is a potential molecular target for the treatment of atherosclerosis. In the present work, natural flavonoids were screened against cathepsin V, and two flavones were identified as potent inhibitors of cathepsin V. On the basis of this result, a combinatorial library of chalcones and flavones was prepared, in solution phase employing a scavenger reagent, and fully evaluated. |
| Databáze: | OpenAIRE |
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