期刊
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
卷 106, 期 38, 页码 16375-16380出版社
NATL ACAD SCIENCES
DOI: 10.1073/pnas.0901310106
关键词
cell death; response to treatment; small animal imaging
资金
- Cancer Research U. K.- Engineering and Physical Sciences Research Council [C2536/A10337]
- U. K. Medical Research Council [U1200.005.00001.01]
- MRC [MC_U120081322] Funding Source: UKRI
- Cancer Research UK [10337] Funding Source: researchfish
- Medical Research Council [MC_U120081322] Funding Source: researchfish
Of the molecular biochemical alterations that occur during apoptosis, activation of caspases, notably caspase-3, is probably the most attractive for developing specific in vivo molecular imaging probes. We recently designed a library of isatin-5 sulfonamides and selected [F-18] ICMT-11 for further evaluation on the basis of subnanomolar affinity for activated capsase-3, high metabolic stability, and facile radiolabeling. In this present study, we have demonstrated that [F-18] ICMT-11 binds to a range of drug-induced apoptotic cancer cells in vitro and to 38C13 murine lymphoma xenografts in vivo by up to 2-fold at 24 h posttreatment compared to vehicle treatment. We further demonstrated that the increased signal intensity in tumors after drug treatment, detected by whole body in vivo microPET imaging, was associated with increased apoptosis. In summary, we have characterized [F-18] ICMT-11 as a caspase-3/7 specific PET imaging radiotracer for the assessment of tumor apoptosis that could find utility in anticancer drug development and the monitoring of early responses to therapy.
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