In vivo imaging of GLP-1R with a targeted bimodal PET/fluorescence imaging agent.
In vivo imaging of GLP-1R with a targeted bimodal PET/fluorescence imaging agent.
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DOI：
10.1021/bc500178d
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发表时间：
2014-07-16
影响因子：
4.7
通讯作者：
Reiner, Thomas
中科院分区：
文献类型：
--
作者：
Brand, Christian;Abdel-Atti, Dalya;Zhang, Yachao;Carlin, Sean;Clardy, Susan M.;Keliher, Edmund J.;Weber, Wolfgang A.;Lewis, Jason S.;Reiner, Thomas
Accurate visualization and quantification of β-cell mass is critical for the improved understanding, diagnosis, and treatment of both type 1 diabetes (T1D) and insulinoma. Here, we describe the synthesis of a bimodal imaging probe (PET/fluorescence) for imaging GLP-1R expression in the pancreas and in pancreatic islet cell tumors. The conjugation of a bimodal imaging tag containing a near-infrared fluorescent dye, and the copper chelator sarcophagine to the GLP-1R targeting peptide exendin-4 provided the basis for the bimodal imaging probe. Conjugation was performed via a novel sequential one-pot synthetic procedure including 64Cu radiolabeling and copper-catalyzed click-conjugation. The bimodal imaging agent 64Cu-E4-Fl was synthesized in good radiochemical yield and specific activity (RCY = 36%, specific activity: 141 μCi/μg, >98% radiochemical purity). The agent showed good performance in vivo and ex vivo, visualizing small xenografts (<2 mm) with PET and pancreatic β-cell mass by phosphor autoradiography. Using the fluorescent properties of the probe, we were able to detect individual pancreatic islets, confirming specific binding to GLP-1R and surpassing the sensitivity of the radioactive label. The use of bimodal PET/fluorescent imaging probes is promising for preoperative imaging and fluorescence-assisted analysis of patient tissues. We believe that our procedure could become relevant as a protocol for the development of bimodal imaging agents.
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影响因子：
62.1
作者：
Louie, Angelique Y.
通讯作者：
Louie, Angelique Y.
影响因子：
64.5
作者：
Pittet MJ;Weissleder R
通讯作者：
Weissleder R
DOI：
10.1073/pnas.1109859108
发表时间：
2011-08-02
影响因子：
11.1
作者：
Reiner, Thomas;Thurber, Greg;Weissleder, Ralph
通讯作者：
Weissleder, Ralph
影响因子：
44.5
作者：
Christ, Emanuel;Wild, Damian;Forrer, Flavio
通讯作者：
Forrer, Flavio
影响因子：
4.7
作者：
Ranyuk, Elena;Lebel, Rejean;Guerin, Brigitte
通讯作者：
Guerin, Brigitte