In vivo evaluation of two tissue transglutaminase PET tracers in an orthotopic tumour xenograft model.

ABSTRACT: BACKGROUND:The protein cross-linking enzyme tissue transglutaminase (TG2; EC 2.3.2.13) is associated with the pathogenesis of various diseases, including cancer. Recently, the synthesis and initial evaluation of two high-potential radiolabelled irreversible TG2 inhibitors were reported by us. In the present study, these two compounds were evaluated further in a breast cancer (MDA-MB-231) tumour xenograft model for imaging active tissue transglutaminase in vivo. RESULTS:The metabolic stability of [11C]1 and [18F]2 in SCID mice was comparable to the previously reported stability in Wistar rats. Quantitative real-time polymerase chain reaction analysis on MDA-MB-231 cells and isolated tumours showed a high level of TG2 expression with very low expression of other transglutaminases. PET imagin

SUBMITTER: van der Wildt B 

PROVIDER: S-EPMC5970127 | biostudies-literature | 2018 May

REPOSITORIES: biostudies-literature