Department of Chemistry, University of Oxford, Chemistry Research Laboratory, Mansfield Road, Oxford OX13TA, UK.
Chembiochem. 2009 Oct 12;10(15):2522-9. doi: 10.1002/cbic.200900425.
Unnatural, NMR- and MRI-active fluorinated sugar probes, designed and synthesised to bind to the pathogenic protein TgMIC1 from Toxoplasma gondii, were found to display binding potency equal to and above that of the natural ligand. Dissection of the binding mechanism and modes, including the first X-ray crystal structures of a fluoro-oligosaccharide bound to a lectin, demonstrate that it is possible to create effective fluorinated probe ligands for the study of, and perhaps intervention in, sugar-protein binding events.
为与刚地弓形虫的致病蛋白 TgMIC1 结合而设计和合成的非天然、NMR 和 MRI 活性氟代糖探针,被发现具有与天然配体相当或更高的结合效力。对结合机制和模式的剖析,包括第一个氟代寡糖与凝集素结合的 X 射线晶体结构,表明有可能为糖蛋白结合事件的研究,甚至干预,创建有效的氟代探针配体。