Novel strategies for ultrahigh specific activity targeted nanoparticles

Zhou, Dong

Washington University, St. Louis, MO

关键词: Radiolabeling;    Targeted Nanoparticles;    Ultrahigh Specific Activity;    38 Radiation Chemistry, Radiochemistry, And Nuclear Chemistry Ultrahigh Specific Activity;   

DOI  :  10.2172/1057282
RP-ID  :  NONE
RP-ID  :  FG02-08ER64671
RP-ID  :  1057282

美国|英语

来源: UNT Digital Library

【 摘 要 】

We have developed novel strategies optimized for preparing high specific activity radiolabeled nanoparticles, targeting nuclear imaging of low abundance biomarkers. Several compounds have been labeled with F-18 and Cu-64 for radiolabeling of SCK-nanoparticles via Copper(I) catalyzed or copper-free alkyne-azide cyclolization. Novel strategies have been developed to achieve ultrahigh specific activity with administrable amount of dose for human study using copper-free chemistry. Ligands for carbonic anhydrase 12 (CA12), a low abundance extracellular biomarker for the responsiveness of breast cancer to endocrine therapie, have been labeled with F-18 and Cu-64, and one of them has been evaluated in animal models. The results of this project will lead to major improvements in the use of nanoparticles in nuclear imaging and will significantly advance their potential for detecting low abundance biomarkers of medical importance.