Department of Diabetes, Endocrinology & Metabolism, Beckman Research Institute of the City of Hope, 1500 East Duarte Road, Duarte, CA 91010, USA.
Curr Pharm Biotechnol. 2010 Sep 1;11(6):572-80. doi: 10.2174/138920110792246564.
Positron emission tomography (PET) is a powerful and rapidly developing area of molecular imaging that is used to study and visualize human physiology by the detection of positron-emitting radiopharmaceuticals. Information about metabolism, receptor/enzyme function, and biochemical mechanisms in living tissue can be obtained directly from PET experiments. In particular, the interest in (18)F-labeled proteins remains high for both diagnoses and therapy monitoring purposes. The development of labeling strategies for the synthesis of new (18)F labeled protein is, however, not trivial. (18)F-containing prosthetic groups are often required for protein labeling to obtain high yield under mild labeling conditions and keep the bioactive character of the proteins. This Review highlights key aspects of protein (18)F-labeling method and discussed representative examples including (18)F-labeled human serum albumin, (18)F-labeled Annexin V, (18)F-labeled HER2 affibody, and (18)F-labeled low density lipoprotein.
正电子发射断层扫描(PET)是分子影像学中一个强大且快速发展的领域,通过检测正电子放射性药物来研究和可视化人体生理学。可以直接从 PET 实验中获得有关代谢、受体/酶功能和生化机制的信息。特别是,(18)F 标记蛋白在诊断和治疗监测方面的应用仍然具有很高的兴趣。然而,开发用于合成新型(18)F 标记蛋白的标记策略并非易事。为了在温和的标记条件下获得高产率并保持蛋白质的生物活性,通常需要(18)F 含有基团作为蛋白质标记的前体。本文综述了蛋白质(18)F 标记方法的关键方面,并讨论了代表性的例子,包括(18)F 标记的人血清白蛋白、(18)F 标记的 Annexin V、(18)F 标记的 HER2 亲和体和(18)F 标记的低密度脂蛋白。