Abstract
We report a first set of peptidomimetic ligands mimicking the adhesive interface identified by recent crystallographic structures of E- and N-cadherin. Compounds 2 and 3 inhibit adhesion of epithelial ovarian cancer (EOC) cells with improved efficacy compared to the ADH-1 peptide, a N-cadherin antagonist that is in early clinical trials in EOC patients.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Cadherins / antagonists & inhibitors*
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Carcinoma, Ovarian Epithelial
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Cell Adhesion / drug effects
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Cell Line, Tumor
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Dose-Response Relationship, Drug
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Drug Design*
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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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Neoplasms, Glandular and Epithelial / drug therapy*
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Neoplasms, Glandular and Epithelial / pathology
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Oligopeptides / chemical synthesis
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Oligopeptides / chemistry
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Oligopeptides / pharmacology*
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Ovarian Neoplasms / drug therapy*
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Ovarian Neoplasms / pathology
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Peptidomimetics*
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Small Molecule Libraries / chemical synthesis
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Small Molecule Libraries / chemistry
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Small Molecule Libraries / pharmacology*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Cadherins
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Ligands
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Oligopeptides
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Peptidomimetics
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Small Molecule Libraries