18F-Labeled Single-Stranded DNA Aptamer for PET Imaging of Protein Tyrosine Kinase-7 Expression

Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine
Orit JacobsonXiaoyuan Chen

Abstract

Protein tyrosine kinase-7 (PTK7), a member of receptor tyrosine kinase superfamily initially identified as colon carcinoma kinase-4, is highly expressed in various human malignancies. Its expression was found to correlate with aggressive biologic behaviors such as increased cell proliferation, invasiveness, and migration. Despite the importance and unmet need of imaging PTK7 in vivo, there is currently no clinically relevant method to visualize tumoral PTK7 expression noninvasively such as PET or SPECT. This study aimed to develop a specific, selective, and high-affinity PET radioligand based on single-stranded DNA aptamer to address this challenge. Sgc8, a 41-oligonucleotide that targets to PTK7, was labeled with (18)F using a 2-step radiochemical synthesis, which featured a direct 1-step radiofluorination on the distinctive spirocyclic hypervalent iodine(III) precursor to give (18)F-fluorobenzyl azide followed by copper-mediated click conjugation with Sgc8-alkyne. (18)F-Sgc8 was evaluated in vitro and in vivo in 2 cell lines, HCT116 and U87MG, which express high and low amounts of PTK7, respectively. Sgc8 was labeled efficiently with (18)F in an isolated radiochemical yield of 62% ± 2%, non-decay-corrected based on (18)F-fluo...Continue Reading

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Citations

Jan 27, 2017·Bioconjugate Chemistry·Guizhi ZhuXiaoyuan Chen
Nov 17, 2017·International Journal of Molecular Sciences·Pascal RöthlisbergerMarcel Hollenstein
Oct 6, 2017·Journal of Labelled Compounds & Radiopharmaceuticals·Victor W Pike
Jul 14, 2017·Chemistry : a European Journal·Hema S KrishnanSteven H Liang
Aug 3, 2018·European Journal of Nuclear Medicine and Molecular Imaging·Siyuan ChengXiaoyuan Chen
May 15, 2020·Cancer Biotherapy & Radiopharmaceuticals·Estefanía SiccoVictoria Calzada
Nov 7, 2020·ACS Applied Materials & Interfaces·Ling Sum LiuPik Kwan Lo
Aug 21, 2018·Advanced Drug Delivery Reviews·Guizhi Zhu, Xiaoyuan Chen
Dec 30, 2017·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Vadim Bernard-GauthierRalf Schirrmacher
May 21, 2021·Bioconjugate Chemistry·Feng LiZheng Li
Oct 16, 2016·ACS Chemical Neuroscience·Zhengxin CaiYiyun Huang
Oct 9, 2021·Scientific Reports·Estefanía SiccoHugo Cerecetto
Dec 10, 2021·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Chang YangHua Naranmandura

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