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 (64)Cu-labeled bioconjugate shows favourable in vitro and in vivo behaviour.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Alkynes / chemistry*
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Alkynes / pharmacokinetics
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Animals
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Azides / chemistry*
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Azides / pharmacokinetics
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Chelating Agents / chemistry*
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Chelating Agents / pharmacokinetics
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Click Chemistry
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Copper / chemistry*
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Copper / pharmacokinetics
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Cycloaddition Reaction
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HCT116 Cells
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Heterocyclic Compounds, 2-Ring / chemistry
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Humans
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Mice
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Neoplasms / metabolism
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Organophosphonates / chemistry
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Somatostatin / analogs & derivatives*
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Somatostatin / chemistry*
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Somatostatin / pharmacokinetics
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Tissue Distribution
Substances
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1,4,8,11-tetraazacyclotetradecane-1-(methanephosphonic acid)-8-(methane carboxylic acid)
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Alkynes
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Azides
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Chelating Agents
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Heterocyclic Compounds, 2-Ring
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Organophosphonates
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Somatostatin
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Copper