18F-labeled proteins

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.