中文摘要：

指向 CEN-1 人的鼻咽的癌(NPC ) 的 dodecapeptide EDIKPKTSLAFR 配体被识别由在 vivo 噬菌体显示。二 tridecapeptides 和他们的衍生物，命名 YR13 ( YEDIKPKTSLAFR )， EY13 ( EDIKPKTSLAFRY )， EY13-NH_2 ( EDIKPKTSLAFRY-NH_2 ) andFmoc-YR13 ( Fmoc-YEDIKPKTSLAFR )，被综合，无线电用~( 131 )标记 I.The 稳定性 invitro ，在忍受 NPC 肿瘤的老鼠的选择噬菌体粒子的简历分发和织物分发被决定，并且无线电的血浆代谢物分析把肽标记被带 out.AlthoughFmoc 和 NH_2 组能保护肽免受 deiodination 的伤害，仅仅 Fmoc 组禁止了 Fmoc-YR13 的绑定到 NPC 肿瘤。复合 EY13-NH_2 ，肽 EY13 的C终端酰胺，有最大的浆液稳定性，最少的 deiodination ，并且证明有利肿瘤/血 ratios.Theselected 噬菌体粒子(噬菌体 3 或噬菌体 5 )是比控制噬菌体(起始的噬菌体显示器肽图书馆)在 NPC 肿瘤集中的更多 .EY13 能也禁止选择噬菌体粒子的绑定到肿瘤。结果显示 EDIKPKTSLAFR 是在诊断、治疗学的 NPC 的一个好候选人。

英文摘要：

A dodecapeptide EDIKPKTSLAFR ligand targeting CEN- 1 human nasopharyngeal carcinoma （NPC） was identified by in vivo phage display. Two tridecapeptides and their derivatives, named YR13 （YEDIKPKTSLAFR）, EY 1 3 （EDIKPKTSLAFRY）, EY 1 3-NH2 （EDIKPKTSLAFRY-NH2） and Fmoc-YR 1 3 （Fmoc-YEDIKPKTSLAFR）, were synthesized and radiolabeled with ^[3]I. The stability in vitro, biodistribution and tissue distribution of selected phage particles in mice bearing NPC tumor were determined, and plasma metabolites analysis of radiolabeled peptides was carried out. Although Fmoc and NH2 groups could protect the peptide from deiodination, only Fmoc group inhibited the binding of Fmoc-YR13 to NPC tumors. The compound EY13-NH2, the C-terminal amide of peptide EY13, had the greatest serum stability, the least deiodination, and showed favorable tumor/blood ratios. The selected phage particles （phage 3 or phage 5） were more concentrated in NPC tumors than the control phage （initial phage display peptide library）. EY13 could also inhibit the binding of selected phage particles to tumors. The results indicated that EDIKPKTSLAFR was a good candidate in diagnostic and therapeutic NPC.