Chelator boosted tumor-retention and pharmacokinetic properties: development of ⁶⁴Cu labeled radiopharmaceuticals targeting neurotensin receptor.

ABSTRACT:

Purpose

Accumulating evidence suggests that neurotensin (NTS) and neurotensin receptors (NTSRs) play key roles in lung cancer progression by triggering multiple oncogenic signaling pathways. This study aims to develop Cu-labeled neurotensin receptor 1 (NTSR1)-targeting agents with the potential for both imaging and therapeutic applications.

Method

A series of neurotensin receptor antagonists (NRAs) with variable propylamine (PA) linker length and different chelators were synthesized, including [⁶⁴Cu]Cu-CB-TE2A-iPA-NRA ([⁶⁴Cu]Cu-4a-c, i = 1, 2, 3), [⁶⁴Cu]Cu-NOTA-2PA-NRA ([⁶⁴Cu]Cu-4d), [⁶⁴Cu]Cu-DOTA-2PA-NRA ([⁶⁴Cu]Cu-4e, also known as [⁶⁴Cu]Cu-3BP-227), and [⁶⁴Cu]Cu-DOTA-VS-2PA-NRA ([⁶

SUBMITTER: Zhang T 

PROVIDER: S-EPMC11368631 | biostudies-literature | 2024 Sep

REPOSITORIES: biostudies-literature