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10.1021/ml300236m

http://scihub22266oqcxt.onion/10.1021/ml300236m
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suck abstract from ncbi


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pmid24900423
      ACS+Med+Chem+Lett 2012 ; 3 (12 ): 1019-23
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  • Strain-Promoted Catalyst-Free Click Chemistry for Rapid Construction of (64)Cu-Labeled PET Imaging Probes #MMPMID24900423
  • Chen K ; Wang X ; Lin WY ; Shen CK ; Yap LP ; Hughes LD ; Conti PS
  • ACS Med Chem Lett 2012[Dec]; 3 (12 ): 1019-23 PMID24900423 show ga
  • A rapid, efficient, and catalyst-free click chemistry method for the construction of (64)Cu-labeled PET imaging probes was reported based on the strain-promoted aza-dibenzocyclooctyne ligation. This new method was exemplified in the synthesis of (64)Cu-labeled RGD peptide for PET imaging of tumor integrin ?v?3 expression in vivo. The catalyst-free click chemistry reaction proceeded with a fast rate and eliminated the contamination problem of the catalyst Cu(I) ions interfering with the (64)Cu radiolabeling procedure under the conventional Cu-catalyzed 1,3-dipolar cycloaddition condition. The new strategy is simple and robust, and the resultant (64)Cu-labeled RGD probe was obtained in an excellent yield and high specific activity. PET imaging and biodistribution studies revealed significant, specific uptake of the "click" (64)Cu-labeled RGD probe in integrin ?v?3-positive U87MG xenografts with little uptake in nontarget tissues. This new approach is versatile, which warrants a wide range of applications for highly diverse radiometalated bioconjugates for radioimaging and radiotherapy.
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