کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9769297 | 1501250 | 2005 | 9 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and evaluation of new tripeptide phosphonate inhibitors of MMP-8 and MMP-2
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
The phosphotryptophan derivative l-Pro-l-Leu-l-(P)Trp(OH)2 (2b) was reported as the first example of left-hand-side1 phosphonate inhibitor of MMP-8. Its uncommon mode of binding to MMP-8 was mainly ascribed to the presence of the proline residue in P3. Ten new analogues of 2b were obtained by replacement of the aminoterminal l-Pro with aminoacid residues bearing small side chains. Most of the new analogues show an increase of affinity for MMP-2 and MMP-8, and different profiles of selectivity. Computer simulations were performed to explain the effects of substitutions on the preferred mode of binding. They reveal that most of the new analogues are probably accommodated in the right, rather than left-hand side of MMP-8 active site.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 40, Issue 3, March 2005, Pages 271-279
Journal: European Journal of Medicinal Chemistry - Volume 40, Issue 3, March 2005, Pages 271-279
نویسندگان
Mariangela Agamennone, Cristina Campestre, Serena Preziuso, Valerio Consalvi, Marcello Crucianelli, Fernando Mazza, Vincenzo Politi, Rino Ragno, Paolo Tortorella, Carlo Gallina,