Part of the Advances in Experimental Medicine and Biology book series (volume 611)
Comparison of [18F]FBA and [18F]FPyMe as peptide radio-labeling agents of PEPHC1 for PET imaging of EGFRvIII
Receptor binding peptides labeled with positron-emitting nuclides for Positron Emission Tomography (PET) are useful targeting agents for diagnostic imaging of various types of cancer. Among the positron emitting nuclides, fluorine-18 is often the radionuclide of choice for labeling of peptides, due to the physical and nuclear characteristics of the isotope [ 1]. A two-step 18F-labeling of resin-bound linear peptides can be achieved by acylation of the N-terminus with 4-[ 18F]fluorobenzoic acid ([ 18F]FBA) [ 2], Figure 1a. Alternatively, 18F-labeling may be performed via the thiol group of cysteine using 1-[3-(2-[ 18F]fluoropyridin-3-yloxy)propyl]pyrrole-2,5-dione ([ 18F]FpyMe) [ 3], Figure 1b. In this study, we compare [ 18F]FBA and [ 18F]FPyMe for the 18F-labeling of PEPHC1 (HFLIIGFMRRALCGA), a peptide which is selective towards the cancer specific epidermal growth factor tyrosine kinase receptor mutation (EGFRvIII) [ 4].
KeywordsRadiochemical Yield Coupling Reagent Growth Factor Tyrosine Kinase Receptor Helix Formation Growth Factor Tyrosine Kinase
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.
The Danish Cancer Society for funding.
The work was funded by an USDA-NRICGP grant to L. Martin.
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