Improvement in the Properties of 3-Phenyl-3-trifluoromethyldiazirine Based Photoreactive Bis-Glucose Probes for GLUT4 Following Substitution on the Phenyl Ring

概要

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We have developed two novel 3-phenyl-3-trifluoromethyldiazirinyl bis-glucose derivatives to investigate the properties of the adipocyte glucose transporter GLUT4. These compounds were substituted by electron-with-drawing (iodo and nitro) groups on the aromatic ring of 3-phenyl-3-tritluoromethyldiazirine photophore and were found to be more photosensitive than compounds without such substituents. The compounds were used as inhibitors of insulin-stimulated glucose transport activity in order to assess half-maximal inhibition or relative affinity values for GLUT4. The affinities were found to be 60-130 times higher than the parent compound D-glu-cose. Because of the increased photo-reactivity and high affinity these compounds will be useful in studies directed at further elucidation of GLUT4 function.
公益社団法人日本薬学会の論文
2002-07-01