Abstract
A siderophore conjugate was designed as a potential PSMA inhibitor and diagnostic agent for prostate cancer. A semi-rigid spacer was incorporated to avoid competitive participation of iron binding by the enzyme inhibitor relative to the siderophore component. Biological test results showed that, even with the extended scaffold, this compound is a potent PSMA inhibitor with an IC50 of 4 nM. This siderophore conjugate may be useful for detection of prostate-derived cancer cells by magnetic resonance imaging (MRI).
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Cross-Linking Reagents
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Drug Design
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology
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Glutamate Carboxypeptidase II / antagonists & inhibitors
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Humans
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Inhibitory Concentration 50
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Magnetic Resonance Imaging
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Male
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Prostate-Specific Antigen / antagonists & inhibitors*
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Prostate-Specific Antigen / chemistry
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Prostatic Neoplasms / diagnosis*
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Siderophores / chemistry*
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Siderophores / pharmacology
Substances
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Cross-Linking Reagents
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Enzyme Inhibitors
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Siderophores
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Glutamate Carboxypeptidase II
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Prostate-Specific Antigen