Abstract
The synthesis of new conformationally biased cyclic pentapeptides, incorporating the RGD sequence, and built around a tetrahydroazoninone scaffold, is reported. They exhibit interesting activity towards integrin alphaVbeta3 and a remarkable selectivity in comparison with integrin alphaVbeta5.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Azo Compounds / chemical synthesis*
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Azo Compounds / pharmacology
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Humans
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Integrin alphaVbeta3 / metabolism
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Integrins / metabolism*
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Ligands
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Molecular Conformation
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Oligopeptides
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Peptides, Cyclic / chemical synthesis*
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Peptides, Cyclic / pharmacology*
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Receptors, Vitronectin / metabolism
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Structure-Activity Relationship
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Substrate Specificity
Substances
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Azo Compounds
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Integrin alphaVbeta3
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Integrins
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Ligands
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Oligopeptides
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Peptides, Cyclic
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Receptors, Vitronectin
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integrin alphaVbeta5
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arginyl-glycyl-aspartic acid