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	潜在的新型肿瘤显像剂~(99)mTc-MAG_3-GGCNGRC的合成及生物分布; Synthesis and biodistribution of a cyclic peptide containing NGR motif as a potential tumor angiogenesis imaging agent
	张弢 ; 王毅 ; 褚泰伟 ; 刘新起 ; 胡少文 ; 王祥云
	2005
关键词	NGR MAG3 CD13 NGR tumor angiogenesis MAG(3) CD13 肿瘤 新生血管
英文摘要	为测评带有NGR基序的小分子多肽的99mTc配合物作为新型肿瘤显像剂的可能性,合成了带双功能螯合剂MAG3的环肽并进行了动物体内分布实验.直链短肽GGCNGRC环化为99mTc-MAG3-GGCNGRC,再与苯甲酰基保护的MAG3的N-羟基琥珀酰亚胺活泼酯偶联,生成Bz-MAG3-GGCNGRC.后者通过氧化-配体交换反应生成9mTc-MAG3-GGCNGRC,其放射化学纯度>90%,在血清和生理盐水中具有较好的稳定性.在正常小鼠和荷瘤裸鼠体内的生物分布表明,此类型小肽通过泌尿系统和肝胆系统代谢.荷直肠癌CL-187的裸鼠模型体内分布显示,注射后3h后,99mTc-MAG3-GGCNGRC,在...; In order to evaluate the potency of short peptides containing NGR motif as the imaging agents for diagnosis of tumor angiogenesis, a preliminary investigation on the synthesis and biodistrubution of a short peptide containing the NGR motif was carried out and the results are reported in the present paper. The open-chain peptide GGCNGRC was first cyclized to GGCNGRC by oxygen oxidation, and then coupled with benzoyl-protected N-hydroxysuccinimidyl-MAG(3) to form Bz-MAG(3)-GGCNGRC. The latter was labeled with Tc-99m by reduction-ligand substitution procedure, while the benzoyl group was removed simultaneously. The labeled complex Tc-99m-MAG(3)-GGCNGRC was isolated by HPLC and purified by reverse-phase sep-pak column. Its radiochemical purity was estimated to be better than 90%. The complex was stable in saline and serum. The biodistribution of Tc-99m-MAG(3)-GGCNGRC in normal and tumor-bearing mice indicates that it is quickly distributed to the whole body and excreted via both hepatobiliary tract and kidney-urethra systems. Tc-99m-MAG(3)-GGCNGRC was accumulated in zenografted colon carcinoma CL-187 after 3 h post injection. It is expected that the radiolabeled short peptides containing NGR motif may be useful as diagnostic imaging agents for tumor angiogenesis.; http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000229296100003&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=8e1609b174ce4e31116a60747a720701 ; SCI(E); 中文核心期刊要目总览(PKU); 中国科技核心期刊(ISTIC); 中国科学引文数据库(CSCD); 1; 05; 801-805; 26
语种	中文
出处	万方 ; 知网 ; SCI
出版者	高等学校化学学报
内容类型	其他
源URL	[http://hdl.handle.net/20.500.11897/79629]
专题	化学与分子工程学院
推荐引用方式 GB/T 7714	张弢,王毅,褚泰伟,等. 潜在的新型肿瘤显像剂~(99)mTc-MAG_3-GGCNGRC的合成及生物分布, Synthesis and biodistribution of a cyclic peptide containing NGR motif as a potential tumor angiogenesis imaging agent. 2005-01-01.

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