Imparting Multivalency to a Bifunctional Chelator: A Scaffold Design for Targeted PET Imaging Probes

Two are better than one: Multivalent scaffolds for targeted PET imaging probes not only feature chelators that form stable and neutral complexes with a radiometal but also contain functional groups for presentation of multiple targeting molecules. A bivalent scaffold was synthesized and coupled with...

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Bibliographic Details
Published in:Angewandte Chemie (International ed.) 2009-01, Vol.48 (40), p.7346-7349
Main Authors: Liu, Wei, Hao, Guiyang, Long, Michael A, Anthony, Tiffani, Hsieh, Jer-Tsong, Sun, Xiankai
Format: Article
Language:English
Subjects:
Animals
Cell Line, Tumor
chelates
Chelating Agents - chemical synthesis
Chelating Agents - chemistry
Drug Design
Humans
imaging agents
Integrin alphaVbeta3 - chemistry
Integrin alphaVbeta3 - metabolism
Mice
multivalent effect
Neoplasms - diagnosis
Oligopeptides - chemistry
Peptides, Cyclic - chemical synthesis
Peptides, Cyclic - chemistry
Positron-Emission Tomography
radiochemistry
Transplantation, Heterologous
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Summary:Two are better than one: Multivalent scaffolds for targeted PET imaging probes not only feature chelators that form stable and neutral complexes with a radiometal but also contain functional groups for presentation of multiple targeting molecules. A bivalent scaffold was synthesized and coupled with a targeting ligand to afford the probe, which was used to efficiently image tumors in vivo (see picture).
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.200903556