| Autor: |
Vassiliou, S. Mucha, A. Cuniasse, P. Georgiadis, D. Lucet-Levannier, K. Beau, F. Kannan, R. Murphy, G. Knäuper, V. Rio, M.-C. Basset, P. Yiotakis, A. Dive, V. |
| Jazyk: |
angličtina |
| Rok vydání: |
1999 |
| Předmět: |
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| Popis: |
Several phosphinic pseudo-tripeptides of general formula R-XaaΨ(PO2- CH2)Xaa'-Yaa'-NH2 were synthesized and evaluated for their in vitro activities to inhibit stromelysin-3, gelatinases A and B, membrane type-1 matrix metalloproteinase, collagenases 1 and 2, and matrilysin. With the exception of collagenase-1 and matrilysin, phosphinic pseudo-tripeptides behave as highly potent inhibitors of matrix metalloproteinases, provided they contain in P1' position an unusual long aryl-alkyl substituent. Study of structure-activity relationships regarding the influence of the R and Xaa' substituents in this series may contribute to the design of inhibitors able to block only a few members of the matrix metalloproteinase family. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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