Abstract
In this paper, we describe the synthesis of a selected library of heterochiral d-Pro-containing RGD-peptidomimetics (RpD) and we investigate the biological activity as inhibitors of fibronectin adhesion to SK-MEL-24 tumor cells. In particular, peptides 4 and 8 showed an IC(50) in the 10(-8)M range. Despite the linear structure, the peptides tend to adopt a folded conformation in a polar environment.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology
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Cell Adhesion / drug effects*
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Cell Line, Tumor
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Fibronectins / metabolism
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Humans
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Inhibitory Concentration 50
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Molecular Mimicry
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Molecular Structure
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Neoplasms / drug therapy
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Neoplasms / pathology*
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Oligopeptides / chemical synthesis
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Oligopeptides / pharmacology*
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Peptide Library
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Proline
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Protein Conformation
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Fibronectins
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Oligopeptides
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Peptide Library
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arginyl-glycyl-aspartic acid
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Proline