Development of a novel radioiodinated glucose derivative with interaction to hexokinase

Abstract

Development of an 123I-labeled glucose derivative that interacted with hexokinase was attempted. By introducing a benzene ring into the glucosamine molecule, we were able to secure a radioiodinated compound, N-iodobenzoyl-D-glucosamine (BGA), with enhanced stability. As a result, a non-competitive inhibitory agent on the hexokinase-regulated phosphorylation reaction was achieved. The inhibitory action and lipophilic property of this novel compound were closely related to an amide bond in its structural configuration. Moreover, on investigating the biodistribution in mice, although this 125I-labeled compound did not display any uptake into the brain, it demonstrated rapid clearance from the blood with high systemic stability. From the above findings, it is highly possible to develop a clinically feasible 123I-labeled radioligand that can monitor the quantitative changes and biodistribution of hexokinase.