Development of anti-EGF receptor peptidomimetics (AERP) as tumor imaging agent.
Development of anti-EGF receptor peptidomimetics (AERP) as tumor imaging agent.
复制标题
开发抗 EGF 受体肽模拟物 (AERP) 作为肿瘤显像剂。
DOI：
10.1016/j.bmcl.2011.02.013
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发表时间：
2011-04-15
影响因子：
2.7
通讯作者：
Murali, Ramachandran
中科院分区：
文献类型：
--
作者：
Ponde, Datta E.;Su, ZiFen;Berezov, Alan;Zhang, Hongtao;Alavi, Abbas;Greene, Mark I.;Murali, Ramachandran
关键词：
EGFR在乳腺癌、前列腺癌、胰腺癌和肺癌等实体瘤中过度表达，并与肿瘤的转移潜能有关。检测了抗EGFR受体结合多肽模拟物(AERP)，以评估该小分子作为肿瘤特异性显像剂的潜在用途。这项工作的目的是设计和表征放射性标记的肽类药物与EGFR过表达的细胞裂解物和A431异种移植瘤的结合特异性。我们新设计的多肽模拟物AERP与DTPA偶联，并用99mTc标记。[99mTC]DTPA-AERP-2体内肿瘤蓄积量为1.6±0.1%ID/g，肿瘤肌肉比为5.5。我们的研究表明，这种新的模拟肽，AERP-2，值得进一步开发为EGFR特异性肿瘤显像剂。
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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DOI：
10.1016/s0360-3016(01)01630-3
发表时间：
2001-10-01
影响因子：
7
作者：
Brizel, DM;Schroeder, T;Mueller-Klieser, W
通讯作者：
Mueller-Klieser, W
影响因子：
4.7
作者：
Lin, KS;Luu, A;Wagner, HN
通讯作者：
Wagner, HN
影响因子：
9.7
作者：
Bell, Andrea;Wang, Zheng J.;Zhang, Jianbing
通讯作者：
Zhang, Jianbing
影响因子：
8
作者：
Liu, BL;Fan, Z
通讯作者：
Fan, Z
影响因子：
1.2
作者：
Suo, ZH;Risberg, B;Nesland, JM
通讯作者：
Nesland, JM