Radiolabelled proteins for positron emission tomography: Pros and cons of labelling methods.
BACKGROUND
Dynamic biomedical research is currently yielding a wealth of information about disease-associated molecular alterations on cell surfaces and in the extracellular space. The ability to visualize and quantify these alterations in vivo could provide important diagnostic information and be used to guide individually-optimized therapy. Biotechnology can provide proteinaceous molecular probes with highly specific target recognitions. Suitably labelled, these may be used as tracers for radionuclide-based imaging of molecular disease signatures. If the labels are positron-emitting radionuclides, the superior resolution, sensitivity and quantification capability of positron emission tomography (PET) can be exploited.


METHODS
This article discusses different approaches to labelling proteins with positron-emitting nuclides with suggestions made depending on the biological features of the tracers.


CONCLUSIONS
Factors such as matching biological and physical half-lives, availability of the nuclide, labelling yields, and influences of labelling on targeting properties (affinity, charge and lipophilicity, cellular processing and retention of catabolites) should be considered when selecting a labelling strategy for each proteinaceous tracer.


CONCLUSIONS
The labelling strategy used can make all the difference between success and failure in a tracer application. This review emphasises chemical, biological and pharmacological considerations in labelling proteins with positron-emitting radionuclides.
Tolmachev
Vladimir
V
Division of Biomedical Radiation Sciences, Rudbeck Laboratory, Uppsala University, SE-75181 Uppsala, Sweden.
Stone-Elander
Sharon
S
D000818:Animals; D006207:Half-Life; D006801:Humans; D007553:Isotope Labeling; D049268:Positron-Emission Tomography / Q000379:methods*; D011506:Proteins / Q000494:pharmacology*; D011849:Radioactive Tracers
D011506:Proteins; D011849:Radioactive Tracers