Laboratory of Bioorganic Chemistry and Crystallography, Faculty of Science and Technology, Free University of Bolzano, Piazza Università 5, 39100 Bolzano, Italy.
Bioorg Med Chem. 2013 Aug 15;21(16):4762-7. doi: 10.1016/j.bmc.2013.05.057. Epub 2013 Jun 5.
In connection with prospective (18)F-PET imaging studies, the potential for enzymatic synthesis of fluorine-labelled glycosides of small molecules was investigated. Approaches to the enzymatic synthesis of anomeric phosphates of d-gluco-configured fluorosugars proved ineffective. In contrast, starting in the d-galacto series and relying on the consecutive action of Escherichia coli galactokinase (GalK), galactose-1-phosphate uridylyltransferase (GalPUT), uridine-5'-diphosphogalactose 4-epimerase (GalE) and oat root glucosyltransferase (SAD10), a quick and effective synthesis of 6-deoxy-6-fluoro-d-glucosyl N-methylanthranilate ester was achieved.
在与前瞻性（18）F-PET 成像研究相关联的研究中，调查了酶促合成小分子氟标记糖苷的可能性。证明酶促合成 d-葡萄糖构型氟糖的端基磷酸酯的方法是无效的。相比之下，从 d-半乳糖系列开始，依靠大肠杆菌半乳糖激酶（GalK）、半乳糖-1-磷酸尿苷酰转移酶（GalPUT）、尿苷-5'-二磷酸半乳糖 4-差向异构酶（GalE）和燕麦根葡糖基转移酶（SAD10）的连续作用，可以快速有效地合成 6-脱氧-6-氟-d-葡糖基 N-甲基邻氨基苯甲酸酯。
