Abstract
Vitronectin receptor (alpha(V)beta(3)) antagonists have been implicated as a possible new treatment of restenosis following balloon angioplasty. In this work we investigate a series of novel arginine mimetic scaffolds leading to new insight of the alpha(V)beta(3)/ligand interaction. Squaric acid amide 10 is a subnanomolar alpha(V)beta(3) antagonist with improved potency on human smooth muscle cell migration.
MeSH terms
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Binding Sites / drug effects
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Biphenyl Compounds / chemistry
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Biphenyl Compounds / pharmacology*
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Cyclobutanes / chemistry
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Cyclobutanes / pharmacology*
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Humans
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Ligands
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Models, Molecular
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Molecular Structure
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Protein Structure, Tertiary
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Receptors, Vitronectin / antagonists & inhibitors*
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Receptors, Vitronectin / chemistry
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Structure-Activity Relationship
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Sulfonamides / chemistry
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Sulfonamides / pharmacology*
Substances
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Biphenyl Compounds
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Cyclobutanes
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Ligands
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Receptors, Vitronectin
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Sulfonamides
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squaric acid amide
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squaric acid dibutyl ester