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The synthesis of pteroyl-lys conjugates and its application as Technetium-99m labeled radiotracer for folate receptor-positive tumor targeting
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
2011-04-01
DOI10.1016/j.bmcl.2011.02.014
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
WOS记录号WOS:000288245100026
项目编号20701004
资助机构National Natural Science Foundation of China
引用统计
被引频次:18[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/65515
专题北京大学临床肿瘤学院
北京大学临床肿瘤学院_核医学科
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
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GB/T 7714
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.
APA Guo, Hongjuan.,Xie, Fang.,Zhu, Meilin.,Li, Yan.,Yang, Zhi.,...&Lu, Jie.(2011).The synthesis of pteroyl-lys conjugates and its application as Technetium-99m labeled radiotracer for folate receptor-positive tumor targeting.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,21(7),2025-2029.
MLA Guo, Hongjuan,et al."The synthesis of pteroyl-lys conjugates and its application as Technetium-99m labeled radiotracer for folate receptor-positive tumor targeting".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 21.7(2011):2025-2029.
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