Phosphinic Pseudo-Tripeptides as Potent Inhibitors of Matrix Metalloproteinases: A Structure−Activity Study
| العنوان: | Phosphinic Pseudo-Tripeptides as Potent Inhibitors of Matrix Metalloproteinases: A Structure−Activity Study |
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| المؤلفون: | Marie-Christine Rio, Philippe Cuniasse, Vera Knäuper, and Athanasios Yiotakis, Dimitris Georgiadis, Gillian Murphy, Paul Basset, Vincent Dive, ‡ Karine Lucet-Levannier, Artur Mucha, Fabrice Beau, Stamatia Vassiliou, Rama Kannan |
| المصدر: | Journal of Medicinal Chemistry. 42:2610-2620 |
| بيانات النشر: | American Chemical Society (ACS), 1999. |
| سنة النشر: | 1999 |
| مصطلحات موضوعية: | Gelatinases, Oligopeptide, Magnetic Resonance Spectroscopy, biology, Phosphines, Stereochemistry, Chemistry, Metalloendopeptidases, Tripeptide, Matrix metalloproteinase, Kinetics, Structure-Activity Relationship, chemistry.chemical_compound, Enzyme inhibitor, Drug Discovery, Peptide synthesis, biology.protein, Molecular Medicine, Structure–activity relationship, Protease Inhibitors, Matrilysin, Oligopeptides |
| الوصف: | Several phosphinic pseudo-tripeptides of general formula R-XaaPsi(PO(2)-CH(2))Xaa'-Yaa'-NH(2) 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 P(1)' 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. |
| تدمد: | 1520-4804 0022-2623 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3708db4988a191221a9dc265cff0e397Test https://doi.org/10.1021/jm9900164Test |
| رقم الانضمام: | edsair.doi.dedup.....3708db4988a191221a9dc265cff0e397 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 15204804 00222623 |
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