Design in silico, synthesis and binding evaluation of a carbohydrate-based scaffold for structurally novel inhibitors of matrix metalloproteinases

被引：18

作者：

Fragai, M

Nativi, C

Richichi, B

Venturi, C

机构：

[1] Univ Florence, Dipartimento Chim Organ Ugo Schiff, I-50019 Sesto Fiorentino, FI, Italy

[2] FiorGen Fdn, Sesto Fiorentino, FI, Italy

[3] Univ Florence, Dept Agr Biotechnol, Sesto Fiorentino, FI, Italy

[4] Univ Florence, Magnet Resonance Ctr, I-50019 Sesto Fiorentino, FI, Italy

[5] ProtEra Srl, Sesto Fiorentino, FI, Italy

来源：

CHEMBIOCHEM | 2005年 / 6卷 / 08期

关键词：

binding; carbohydrates; inhibitors; metalloproteinases; NMR spectroscopy; structure-activity relationships;

D O I：

10.1002/cbic.200400456

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 [生物化学与分子生物学]; 081704 [应用化学];

摘要：

Bicyclic α-O-glycodipeptide mimetic scaffolds have been designed, synthesized and tested as new inhibitors of matrix metalloproteinases (MMPs). These compounds exhibit a wide synthetic versatility, suitable water solubility and peculiar bioavailability properties. The interaction with MMP-12, predicted by molecular docking (model shown), was assessed by NMR and fluorimetric assay. © 2005 Wiley-VCH Verlag GmbH & Co. KGaA.

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页码：1345 / 1349

页数：5

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