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Bioorg Med Chem Lett. 2011 Apr 15;21(8):2550-3. doi: 10.1016/j.bmcl.2011.02.013. Epub 2011 Feb 15.

Development of anti-EGF receptor peptidomimetics (AERP) as tumor imaging agent.

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  • 1Department of Radiology, Cyclotron Facility, 420 Curie Blvd., University of Pennsylvania, Philadelphia, PA 19104, United States.


EGFR is over-expressed in several solid tumors including breast, prostate, pancreas, and lung cancers and is correlated to the metastatic potential of the tumor. Anti-EGFR receptor-binding peptidomimetics (AERP) were examined to assess the small molecule's potential use as tumor-specific imaging agents. The aim of this work was to design and characterize the binding specificity of the radiolabeled peptidomimetics to EGFR over-expressing cell lysate and to A431 xenograft tumors. Our newly designed peptidomimetic, AERP, was conjugated to DTPA and labeled with (99m)Tc. The in vivo tumor accumulation of [(99m)Tc] DTPA-AERP-2 was 1.6±0.1%ID/g and tumor to muscle ratio was 5.5. Our studies suggest that this novel peptidomimetic, AERP-2, warrants further development as an EGFR specific tumor-imaging agent.

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