Abstract
The first macrocyclic bifunctional chelator incorporating propylene cross-bridge was efficiently synthesized from cyclam in seven steps. After the introduction of an extra functional group for facile conjugation onto the propylene cross-bridge, the two carboxylic acid pendants could contribute to strong coordination of Cu(II) ions, leading to a robust Cu complex. The cyclic RGD peptide conjugate of PCB-TE2A-NCS was prepared and successfully radiolabeled with (64)Cu ion. The radiolabeled peptide conjugate was evaluated in vivo through a biodistribution study and animal PET imaging to demonstrate high tumor uptake with low background.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Alkenes / chemistry*
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Animals
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Chelating Agents / chemical synthesis
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Chelating Agents / chemistry*
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Chelating Agents / pharmacokinetics
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Coordination Complexes / chemistry
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Copper / chemistry*
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Copper Radioisotopes / chemistry
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Copper Radioisotopes / pharmacokinetics
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Drug Design*
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Glioblastoma / metabolism
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Glioblastoma / pathology
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Heterocyclic Compounds / chemistry
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Humans
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Macrocyclic Compounds / chemical synthesis
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Macrocyclic Compounds / chemistry*
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Mice
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Mice, Nude
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Models, Chemical
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Molecular Structure
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Oligopeptides / chemistry
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Positron-Emission Tomography / methods
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Rats
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Tissue Distribution
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Transplantation, Heterologous
Substances
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Alkenes
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Chelating Agents
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Coordination Complexes
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Copper Radioisotopes
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Heterocyclic Compounds
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Macrocyclic Compounds
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Oligopeptides
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cyclam
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Copper
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arginyl-glycyl-aspartic acid
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propylene