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KMID : 1148920100440030185
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Nuclear Medicine and Molecular Imaging
2010 Volume.44 No. 3 p.185 ~ p.192
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A New Synthesis of TE2A?a Potential Bifunctional Chelator for 64Cu
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Pandya Darpan N.
Kim Jung-Young
Kwak Won-Jung
Park Jeong-Chan
Gawande Manoj B.
An Gwang-Il
Ryu Eun-Kyoung
Yoo Jeong-Soo
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Abstract
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Purpose: The development of a new bifunctional chelator, which holds radiometals strongly in living systems, is a prerequisite for the successful application of disease-specific biomolecules to medical diagnosis and therapy. Recently, TE2A was reported to make kinetically more stable Cu(II) complexes than TETA. Herein, we report a new synthetic route to TE2A and explore its potential as a bifunctional chelator.
Methods: TE2A was synthesized using the regioselective alkylation of benzyl bromoacetate and successive deprotection of the methylene bridge and benzyl group. Salt-free TE2A was radiolabeled with 64Cu and microPET imaging was performed to follow the clearance pattern of the 64Cu-TE2A complex. TE2A was conjugated with cyclic RGD peptide and the TE2A-c(RGDyK) conjugate was radiolabeled with 64Cu.
Results: TE2A was prepared in salt-free form from cyclam in an overall yield of 74%. The microPET images showed that 64Cu-TE2A is excreted rapidly from the body by the kidney and liver. TE2A was successfully conjugated with c(RGDyK) peptide through one carboxylate group and the TE2A-c(RGDyK) conjugate was radiolabeled with 64Cu in 94% yield within 30 min.
Conclusion: TE2A can be used by itself as a bifunctional chelator without any further structural modification.
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KEYWORD
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TE2A, Bifunctional chelator, 64Cu, Conjugation, RGD peptide
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