Synthesis, radiolabeling, and evaluation of 68Ga-labeled aminoquinoxaline derivative as a potent PFKFB3-targeted PET tracer.

ABSTRACT: Glycolysis, as a multi-step oxidation process, plays important roles in the energy supply for living cells, including malignant tumor cells. Recent studies have revealed that 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (named PFKFB3), a bifunctional enzyme in glycolysis, is upregulated in a variety of malignant solid tumors and has been regarded as a potential biomarker for the diagnosis and treatment of tumor patients. Based on the structure of selective PFKFB3 inhibitors, we designed and synthesized a radio-metal radiolabeled small molecule, ⁶⁸Ga-5, which also showed potent selectivity in enzymatic and biochemical tests (with an IC₅₀ value of 12.5 nM). According to further in vitro and in vivo evaluations, ⁶⁸Ga-5 showed promising p

SUBMITTER: Chen F 

PROVIDER: S-EPMC10073729 | biostudies-literature | 2023

REPOSITORIES: biostudies-literature