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Issue 9, 2015
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Cu(i)-assisted click chemistry strategy for conjugation of non-protected cross-bridged macrocyclic chelators to tumour-targeting peptides

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Abstract

Copper(I)-catalyzed azide–alkyne cycloaddition (CuAAC) click chemistry has inherent challenges for copper-labeled radiopharmaceuticals. An azide-modified phosphonate-based cross-bridged macrocyclic chelator was synthesized for click chemistry conjugation with azide-modified Y3-TATE (a somatostatin analogue) on resin, without the need for protecting the chelator. The 64Cu-labeled bioconjugate shows favourable in vitro and in vivo behaviour.

Graphical abstract: Cu(i)-assisted click chemistry strategy for conjugation of non-protected cross-bridged macrocyclic chelators to tumour-targeting peptides

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Supplementary files

Article information


Submitted
17 Dec 2014
Accepted
23 Jan 2015
First published
27 Jan 2015

Dalton Trans., 2015,44, 3945-3948
Article type
Communication
Author version available

Cu(I)-assisted click chemistry strategy for conjugation of non-protected cross-bridged macrocyclic chelators to tumour-targeting peptides

Z. Cai, B. T. Y. Li, E. H. Wong, G. R. Weisman and C. J. Anderson, Dalton Trans., 2015, 44, 3945
DOI: 10.1039/C4DT03897E

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