Evaluation of Pan-SSTRs Targeted Radioligand [64Cu]NOTA-PA1 Using Micro-PET Imaging in Xenografted Mice | Zendy

Fei Liu | Zendy; Xiaoyi Guo | Zendy; Teli Liu | Zendy; Xiaoxia Xu | Zendy; Nan Li | Zendy; Chiyi Xiong | Zendy; Chun Li | Zendy; Hua Zhu | Zendy; Zhi Yang | Zendy

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Evaluation of Pan-SSTRs Targeted Radioligand [⁶⁴Cu]NOTA-PA1 Using Micro-PET Imaging in Xenografted Mice

Author(s) -

Fei Liu,

Xiaoyi Guo,

Teli Liu,

Xiaoxia Xu,

Nan Li,

Chiyi Xiong,

Chun Li,

Hua Zhu,

Zhi Yang

Publication year - 2020

Publication title -

acs medicinal chemistry letters

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.065

H-Index - 66

ISSN - 1948-5875

DOI - 10.1021/acsmedchemlett.9b00544

Subject(s) - biodistribution , somatostatin receptor , radiosynthesis , in vivo , somatostatin , radioligand , chemistry , octreotide , nuclear medicine , molecular imaging , preclinical imaging , in vitro , cancer research , positron emission tomography , medicine , biochemistry , biology , microbiology and biotechnology

64 Cu-labeled new pan-somatostatin receptors (pan-SSTRs) probe PA1 was synthesized, characterized, and evaluated by in vitro and in vivo experiments. [ 64 Cu]NOTA-PA1 was obtained with high specific activity, high radiochemical purity, and good stability. Cell uptake of [ 64 Cu]NOTA-PA1 was higher than that of [ 64 Cu]DOTA-TATE in MCF-7, A549, BGC823, and HT-29 cell lines. [ 64 Cu]NOTA-PA1 showed high binding affinity for SSTRs expressed in A549 cells. The in vivo biodistribution and micropositron emission tomography (micro-PET) imaging studies of [ 64 Cu]NOTA-PA1 revealed good detection ability in MCF-7 and A549 xenografted nude mice. The radiosynthesis, quality control, and preliminary biological evaluation of [ 64 Cu]NOTA-PA1 have broaden the application of radiolabeled octreotide for SSTRs imaging, which could act as a potential multisubtypes targeted radiotracer for imaging SSTRs-positive tumors.

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