A Clinical PET Imaging Tracer ([¹⁸F]DASA-23) to Monitor Pyruvate Kinase M2-Induced Glycolytic Reprogramming in Glioblastoma.

ABSTRACT:

Purpose

Pyruvate kinase M2 (PKM2) catalyzes the final step in glycolysis, a key process of cancer metabolism. PKM2 is preferentially expressed by glioblastoma (GBM) cells with minimal expression in healthy brain. We describe the development, validation, and translation of a novel PET tracer to study PKM2 in GBM. We evaluated 1-((2-fluoro-6-[¹⁸F]fluorophenyl)sulfonyl)-4-((4-methoxyphenyl)sulfonyl)piperazine ([¹⁸F]DASA-23) in cell culture, mouse models of GBM, healthy human volunteers, and patients with GBM.

Experimental design

[¹⁸F]DASA-23 was synthesized with a molar activity of 100.47 ± 29.58 GBq/μmol and radiochemical purity >95%. We performed initial testing of [¹⁸F]DASA-23 in GBM cell culture and human GBM xenografts implanted

SUBMITTER: Beinat C 

PROVIDER: S-EPMC8639752 | biostudies-literature | 2021 Dec

REPOSITORIES: biostudies-literature