Dejesus Onofre T
School of Medicine and Public Health, University of Wisconsin-Madison, B1316 Wisconsin Institutes for Medical Research (WIMR), Madison, WI 53705, USA.
Curr Radiopharm. 2012 Jan;5(1):15-8. doi: 10.2174/1874471011205010015.
Epidermal growth factor receptors (EGFR) are over-expressed in many different types of cancer, thus, are logical targets for both diagnosis and therapy. Antibodies and antibody fragments targeting the extracellular EGF receptor and small molecules targeting the intracellular tyrosine kinase (TK) part of EGFR have been developed as possible diagnostic EGFR imaging agents. Recently, a 12-amino acid peptide, GE11, was identified using phage display screening to have high affinity for EGFR (Kd=22nM). Reported in vitro and in vivo characteristics of GE11 suggest that positron-labeled GE11 may be a useful PET imaging agent in selecting patients with EGFR-rich tumors who can most benefit from anti- EGFR therapy. To enable the exploration of this possibility, positron emitting [64Cu]Cu-NOTA-Bn-GE11 was prepared for further evaluation as PET EGFR imaging agent.
表皮生长因子受体（EGFR）在许多不同类型的癌症中过度表达，因此，它是诊断和治疗的合理靶点。针对细胞外EGF受体的抗体和抗体片段以及针对EGFR细胞内酪氨酸激酶（TK）部分的小分子已被开发为可能的EGFR诊断成像剂。最近，通过噬菌体展示筛选鉴定出一种12个氨基酸的肽GE11，它对EGFR具有高亲和力（Kd = 22nM）。GE11的体外和体内特性表明，正电子标记的GE11可能是一种有用的PET成像剂，可用于选择那些能从抗EGFR治疗中获益最大的富含EGFR肿瘤患者。为了探索这种可能性，制备了发射正电子的[64Cu]Cu-NOTA-Bn-GE11，作为PET EGFR成像剂进行进一步评估。
