Journal article
Gallium-68 complex of a macrobicyclic cage amine chelator tethered to two integrin-targeting peptides for diagnostic tumor imaging
MT Ma, OC Neels, D Denoyer, P Roselt, JA Karas, DB Scanlon, JM White, RJ Hicks, PS Donnelly
Bioconjugate Chemistry | AMER CHEMICAL SOC | Published : 2011
DOI: 10.1021/bc200319q
Abstract
Tumor-targeting peptides radiolabeled with positron-emitting 68Ga are promising candidates as new noninvasive diagnostic agents for positron emission tomography (PET). The targeting peptides are tethered to a chelator that forms a stable coordination complex with Ga3+ that is inert to dissociation of Ga3+in vivo. Metal complexes of macrobicyclic hexaamine "sarcophagine" (sar = 3,6,10,13,16,19- hexaazabicyclo[6.6.6]icosane) ligands exhibit remarkable stability as a result of the encapsulating nature of the cage amine ligand. A Ga3+ sarcophagine complex, [Ga-(1-NH3-8-NH2-sar)]4+, has been characterized using X-ray crystallography, demonstrating that Ga 3+ is coordinated to six nitrogen atoms i..
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Funding Acknowledgements
M.T.M. acknowledges Cancer Council Victoria for providing a Sydney Parker Smith Postdoctoral Cancer Research Fellowship; a Kaye Merlin Brutton Bequest. P.S.D. acknowledges funding from the Australian Research Council and National Health and Medical Research Council. The authors thank Dr. N. Pouliot from the Metastasis Research Lab at The Peter MacCallum Cancer Centre for gifting 66cl4 beta 3 and 66c14pBabe cells, Dr. Peter Eu for helpful discussions, Mr. Wayne Noonan for assistance with HPLC, Mr. David Muller from the Cancer Epidemiology Centre, Cancer Council Victoria for statistical analyses, and Dr. Brett Paterson for proof reading the manuscript.