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Production of 64Cu-labeled monobody for imaging of human EphA2-expressing tumors.

Abstract：

:We previously reported on the monobody E1, which specifically targets the tumor marker hEphA2. In this study, we labeled NOTA-conjugated E1 with 64Cu (64Cu-NOTA-E1) and evaluated biologic characteristics. The uptake of 64Cu-NOTA-E1 in PC3 cells (a human prostate cancer cell line) with high expression of hEphA2 increased in a time-dependent manner. In PC3 xenograft mice, 64Cu-NOTA-E1 injected via the tail vein allowed visualization of tumors on positron emission tomography after 1 h and the highest uptake measured at 24 h post-injection. By contrast, the radioactivity of other tissues either did not increase or decreased over 24 h. This indicates that 64Cu-NOTA-E1 has high tumor uptake and retention, with rapid clearance, and low background values in other tissues. Therefore, 64Cu-NOTA-E1 should be suitable as a novel PET imaging agent for hEphA2-expressing tumors.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Pyo A,You SH,Sik Kim H,Young Kim J,Min JJ,Kim DY,Hong Y

doi

10.1016/j.bmcl.2020.127262

subject

Has Abstract

pub_date

2020-07-15 00:00:00

pages

127262

issue

14

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(20)30367-X

journal_volume

30

pub_type

杂志文章

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