Tyrosine Kinase Inhibitors Reduce Glucose Uptake by Binding to an Exofacial Site on hGLUT-1: Influence on ¹⁸ F-FDG PET Uptake.

ABSTRACT: Positron emission tomography (PET) using 2-deoxy-2-[¹⁸ F]fluoro-d-glucose ([¹⁸ F]FDG), a marker of energy metabolism and cell proliferation, is routinely used in the clinic to assess patient response to chemotherapy and to monitor tumor growth. Treatment with some tyrosine kinase inhibitors (TKIs) causes changes in blood glucose levels in both nondiabetic and diabetic patients. We evaluated the interaction of several classes of TKIs with human glucose transporter-1 (hGLUT-1) in FaDu and GIST-1 cells by measuring [³ H]2-deoxy-d-glucose ([³ H]2-DG) and [³ H]FDG uptake. Uptake of both was inhibited to varying extents by the TKIs, and representative TKIs from each class showed competitive inhibition of [³ H]2-DG uptake. In GIST-

SUBMITTER: Damaraju VL 

PROVIDER: S-EPMC8212708 | biostudies-literature | 2021 May

REPOSITORIES: biostudies-literature