Development of anti-EGF receptor peptidomimetics (AERP) as tumor imaging agent |
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Authors: | Ponde Datta E Su ZiFen Berezov Alan Zhang Hongtao Alavi Abbas Greene Mark I Murali Ramachandran |
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Institution: | a Department of Pathology and Laboratory Medicine, 3620 Hamilton Walk, University of Pennsylvania, Philadelphia, PA 19104, United States b Department of Radiology, Cyclotron Facility, 420 Curie Blvd., University of Pennsylvania, Philadelphia, PA 19104, United States c Institute of Nuclear Science and Technology, Sichuan University, Chengdu, Sichuan 610064, China |
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Abstract: | EGFR is over-expressed in several solid tumors including breast, prostate, pancreas, and lung cancers and is correlated to the metastasic 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 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. Our studies suggest that this novel peptidomimetic, AERP-2, warrants further development as an EGFR specific tumor-imaging agent. |
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Keywords: | Radiolabeled peptidomimetics and peptide AERP-2 Technetium-99m EGFR c-erbB2 Tyrosine kinase receptors EGFR specific radiotracer |
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