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学科主题: 临床医学
题名:
The synthesis of pteroyl-lys conjugates and its application as Technetium-99m labeled radiotracer for folate receptor-positive tumor targeting
作者: Guo, Hongjuan1; Xie, Fang1; Zhu, Meilin1; Li, Yan1,2; Yang, Zhi2; Wang, Xuebin1; Lu, Jie1
关键词: (99m)Tc ; Folate receptor ; Folate-drug conjugates ; Pteroyl-lys-HYNIC ; Tumor imaging
刊名: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
发表日期: 2011-04-01
DOI: 10.1016/j.bmcl.2011.02.014
卷: 21, 期:7, 页:2025-2029
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]: Pharmacology & Pharmacy ; Chemistry
关键词[WOS]: PRECLINICAL EVALUATION ; FOLIC-ACID ; IN-VIVO ; IMAGING AGENTS ; CELL-LINES ; DERIVATIVES ; DELIVERY ; ISOFORMS ; THERAPY ; TISSUES
英文摘要:

Aiming to develop a new (99m)Tc-labeled folate derivative for FR-positive tumor imaging, a simpler method has been established to synthesize the folate-drug conjugates with free alpha-carboxyl group. In this study, the conjugate pteroyl-lys-HYNIC was synthesized and labeled with (99m)Tc using tricine and TPPTS as co-ligands. The radiochemical purity of the final complex (99m)Tc(HYNIC-lys-pteroyl)(tricine/TPPTS), 5 was high (>98%), and it remained stable in saline and plasma over 6 h after preparation. The biologic evaluation results showed that the (99m)Tc labeled pteroyl-lys conjugate was able to specifically target the FR-positive tumor cells and tissues both in vitro and in vivo, highlighting its potential as an effective folate receptor targeted agent for tumor imaging. (C) 2011 Elsevier Ltd. All rights reserved.

语种: 英语
所属项目编号: 20701004
项目资助者: National Natural Science Foundation of China
WOS记录号: WOS:000288245100026
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/65515
Appears in Collections:北京大学临床肿瘤学院_期刊论文

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作者单位: 1.Beijing Normal Univ, Coll Chem, Minist Educ, Key Lab Radiopharmaceut, Beijing 100875, Peoples R China
2.Peking Univ, Sch Oncol, Breast Ctr,Beijing Canc Hosp & Inst, Minist Educ,Key Lab Carcinogenesis & Translat Res, Beijing 100142, Peoples R China

Recommended Citation:
Guo, Hongjuan,Xie, Fang,Zhu, Meilin,et al. The synthesis of pteroyl-lys conjugates and its application as Technetium-99m labeled radiotracer for folate receptor-positive tumor targeting[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2011,21(7):2025-2029.
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