Abstract:
:To develop a radioactive metal complex platform for tumor theranostics, we introduced three radiopharmaceutical derivatives of 1,4,7,10-tetraazacyclododecane-1,4,7-trisacetic acid-benzothiazole aniline (DO3A-BTA, L1) labeled with medical radioisotopes for diagnosis (68Ga/64Cu) and therapy (177Lu). The tumor-targeting ability of these complexes was demonstrated in a cellular uptake experiment, in which 177Lu-L1 exhibited markedly higher uptake in HeLa cells than the 177Lu-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid complex. According to in vivo positron emission tomography imaging, high accumulation of 68Ga-L1 and 64Cu-L1 was clearly visualized in the tumor site, while 177Lu-L1 showed therapeutic efficacy in therapy experiments. Consequently, this molecular platform represents a useful approach in nuclear medicine toward tumor-theranostic radiopharmaceuticals when 68Ga-L1 or 64Cu-L1 is used for diagnosis, 177Lu-L1 is used for therapy, or two of the compounds are used in conjunction with each other.
journal_name
Mol Pharmjournal_title
Molecular pharmaceuticsauthors
Park JA,Lee JW,Kim HK,Shin UC,Lee KC,Kim TJ,Chang Y,Kim KM,Kim JY,Lee YJdoi
10.1021/acs.molpharmaceut.7b00996subject
Has Abstractpub_date
2018-03-05 00:00:00pages
1133-1141issue
3eissn
1543-8384issn
1543-8392journal_volume
15pub_type
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