Radiolabelled proteins for positron emission tomography: Pros and cons of labelling methods

Vladimir Tolmachev, Sharon Stone-Elander

Research output: Contribution to journalReview articlepeer-review

64 Citations (Scopus)

Abstract

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. Scope of review: This article discusses different approaches to labelling proteins with positron-emitting nuclides with suggestions made depending on the biological features of the tracers. Major 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. General significance: 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.

Original languageEnglish
Pages (from-to)487-510
Number of pages24
JournalBiochimica et Biophysica Acta - General Subjects
Volume1800
Issue number5
DOIs
Publication statusPublished - May 2010
Externally publishedYes

Keywords

  • Antibody
  • Labelling
  • Peptide
  • Positron emission tomography
  • Protein
  • Radionuclide

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology

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