Department of Radiology, Cyclotron Facility, 420 Curie Blvd., University of Pennsylvania, Philadelphia, PA 19104, United States.
Bioorg Med Chem Lett. 2011 Apr 15;21(8):2550-3. doi: 10.1016/j.bmcl.2011.02.013. Epub 2011 Feb 15.
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.
表皮生长因子受体在多种实体瘤中过度表达，包括乳腺癌、前列腺癌、胰腺癌和肺癌，并且与肿瘤的转移潜力相关。针对表皮生长因子受体结合的肽模拟物（AERP）进行了检查，以评估小分子作为肿瘤特异性成像剂的潜在用途。本工作旨在设计和表征放射性标记的肽模拟物与 EGFR 过表达细胞裂解物和 A431 异种移植肿瘤的结合特异性。我们新设计的肽模拟物 AERP 与 DTPA 缀合并用 (99m)Tc 标记。[(99m)Tc]DTPA-AERP-2 的体内肿瘤积累为 1.6±0.1%ID/g，肿瘤与肌肉的比值为 5.5。我们的研究表明，这种新型肽模拟物 AERP-2 有进一步开发为 EGFR 特异性肿瘤成像剂的潜力。
