Development of anti-EGF receptor peptidomimetics (AERP) as tumor imaging agent
Graphical abstract
In certain human cancers, EGFR is over-expressed and is related to the metastasic potential of the tumor. We have developed two anti-EGFR receptor-binding peptidomimetics (AERP), as tumor-specific imaging agents. Our newly designed peptidomimetic, AERP, was conjugated to DTPA and labeled with 99mTc. The in vivo tumor accumulation of [99mTc] DTPA-AERP-2 was 1.6 ± 0.1 %ID/g and tumor to muscle ratio was 5.5.
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Acknowledgments
Authors would like to thank Drs. Kathy Valantine and Josh Wand, Department of biophysics and biochemistry of University of Pennsylvania for providing the solution structure of AERP. This work was partly supported by grants from Society for Nuclear Medicine (R.M.), NIH (5P01 CA089480-03) to R.M. and M.I.G., and by grants from Susan G. Komen Breast Cancer Foundation to R.M. (IMG0201367).
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Present address: Department of Biomedical Sciences, Cedars-Sinai Medical Center, Los Angeles, CA 90048, United States.