PET imaging of PARP expression using ⁶⁸Ga-labelled inhibitors.

ABSTRACT:

Purpose

Imaging the PARP expression using ¹⁸F probes has been approved in clinical trials. Nevertheless, hepatobiliary clearance of both ¹⁸F probes hindered their application in monitoring abdominal lesions. Our novel ⁶⁸Ga-labelled probes aim for fewer abdominal signals while ensuring PARP targeting by optimizing the pharmacokinetic properties of radioactive probes.

Methods

Three radioactive probes targeted PARP were designed, synthesized, and evaluated based on the PARP inhibitor Olaparib. These ⁶⁸Ga-labelled radiotracers were assessed in vitro and in vivo.

Results

Precursors that did not lose binding affinity for PARP were designed, synthesized, and then labelled with ⁶⁸Ga in high radiochemical purity (> 97%). T

SUBMITTER: Wang X 

PROVIDER: S-EPMC10317875 | biostudies-literature | 2023 Jul

REPOSITORIES: biostudies-literature