Abstract
As our ongoing work, a series of peptidomimetic L-iso-glutamine derivatives derived from antineoplaston AS2-5 scaffold were prepared and their APN/CD13 and MMP-2 inhibitory activities were evaluated hereby. The results displayed that these compounds exhibited selective inhibition against APN as compared with MMP-2, with IC(50) values in micromole range. Compounds A1 and A2 showed comparable APN inhibitory activities than the positive control bestatin.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Binding Sites
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CD13 Antigens / antagonists & inhibitors*
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CD13 Antigens / chemistry
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Glutamine / analogs & derivatives*
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Glutamine / chemistry
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Glutamine / pharmacology
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Humans
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Inhibitory Concentration 50
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Models, Molecular
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Phenylacetates / chemistry
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Phenylacetates / pharmacology*
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Protease Inhibitors / chemistry
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Protease Inhibitors / pharmacology*
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Phenylacetates
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Protease Inhibitors
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Glutamine
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CD13 Antigens