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.jpg): Failed to open stream: No such file or directory in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 117 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.