Fluoro-pegylated (FPEG) imaging agents targeting Aβ aggregates
Fluoro-pegylated (FPEG) imaging agents targeting Aβ aggregates
复制标题
DOI：
10.1021/bc060239q
复制
发表时间：
2007-01-01
影响因子：
4.7
通讯作者：
Kung, Hank F.
中科院分区：
文献类型：
--
作者：
Stephenson, Karin A.;Chandra, Rajesh;Kung, Hank F.
报道了一种通过基于聚乙二醇化-聚乙二醇化（FPEG）策略形成生物缀合物来生产正电子发射断层扫描（PET）成像剂的新方法。这种方法提供了一种简单易行的方法，通过该方法将F-18掺入靶分子中，而亲脂性没有明显增加。在F-18标记后，这种方便的方法导致PET成像探针使用已知的核心结构，如[2-（4-二甲基氨基苯基）-乙烯基]-苯并恶唑（3 '）或2-苯基苯并噻唑（4），与脑中的A β聚集体（与阿尔茨海默病相关的重要因素）结合。这种方法在某些核心结构中似乎是有效的，但它不能统一地应用于所有结构。
A novel approach of producing positron emission tomography (PET) imaging agents through the formation of bioconjugates based on a pegylation-fluorination strategy resulting in fluoro-pegylated (FPEG) molecules is reported. This approach offers a simple and easy method by which to incorporate F-18 in the target molecule without an appreciable increase in the lipophilicity. After F-18 labeling, this convenient approach leads to PET imaging probes binding to A beta aggregates in the brain (an important factor associated with Alzheimer's disease) using the known core structures, such as [2-(4-dimethylaminophenyl)-vinyl]-benzoxazol (3') or 2-phenylbenzothiazole (4). This approach appears to be effective in some core structures, but it cannot be uniformly applied to all structures.