Design, synthesis and preliminary biological evaluation of a focused combinatorial library of stereodiverse carbohydrate-scaffold-based peptidomimetics.
A focused combinatorial library of 126 mimetics of the RGD sequence based on sugar scaffolds have been rationally constructed using molecular modeling, with a particular emphasis on the stereodiversity of the library. A liquid phase, mix and divide synthesis was used, active compounds being identified by using orthogonal libraries and recursive deconvolution strategies.
Groupe SUCRES, Unité Mixte 7565 CNRS-Université Henri Poincaré-Nancy 1, Nancy-Vandoeuvre, France.
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Moitessier
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Dufour
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Chrétien
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JP
Thiery
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B
Maigret
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Chapleur
D000818:Animals; D001667:Binding, Competitive; D002241:Carbohydrates / Q000737:chemistry; D002448:Cell Adhesion / Q000187:drug effects; D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D015195:Drug Design; D005353:Fibronectins / Q000378:metabolism; D051379:Mice; D008958:Models, Molecular; D018716:Molecular Mimicry; D009842:Oligopeptides / Q000138:chemical synthesis / Q000737:chemistry; D010455:Peptides / Q000737:chemistry; D019030:Receptors, Vitronectin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D012509:Sarcoma / Q000473:pathology; D013237:Stereoisomerism; D014407:Tumor Cells, Cultured / Q000187:drug effects; D019096:Vitronectin / Q000378:metabolism
D002241:Carbohydrates; D005353:Fibronectins; D009842:Oligopeptides; D010455:Peptides; D019030:Receptors, Vitronectin; D019096:Vitronectin; C047981:arginyl-glycyl-aspartic acid