Development of [¹⁸F]DASA-10 for enhanced imaging of pyruvate kinase M2.

ABSTRACT:

Purpose

The aim of this study was to develop a positron emission tomography (PET) radiotracer for measuring pyruvate kinase M2 (PKM2) with improved physicochemical and pharmacokinetic properties compared to [¹⁸F]DASA-23.

Experimental design

First, we synthesized [¹⁸F]DASA-10 and tested its uptake and retention compared to [¹⁸F]DASA-23 in human and mouse glioma cell lines. We then confirmed the specificity of [¹⁸F]DASA-10 by transiently modulating the expression of PKM2 in DU145 and HeLa cells. Next, we determined [¹⁸F]DASA-10 pharmacokinetics in healthy nude mice using PET imaging and subsequently assessed the ability of [¹⁸F]DASA-10 versus [¹⁸F]DASA-23 to enable in vivo detection of intracranial gl

SUBMITTER: Kendirli MT 

PROVIDER: S-EPMC10843576 | biostudies-literature | 2023 Sep-Oct

REPOSITORIES: biostudies-literature