| 孙夕林 王凯 赵周社 李宏利 孙莹莹 申宝忠.18F标记表皮生长因子受体酪氨酸激酶抑制剂4-苯氨基- 喹唑啉
类方法进展[J].现代生物医学进展英文版,2014,14(3):597-600. |
| 18F标记表皮生长因子受体酪氨酸激酶抑制剂4-苯氨基- 喹唑啉
类方法进展 |
| Method Progress of 18F Labeled EGFR-TK inhibitorof 4-anilino-quinazoline |
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| DOI： |
| 中文关键词: 18F 表皮生长因子受体酪氨酸激酶抑制剂 4-苯氨基- 喹唑啉类 |
| 英文关键词: 18F biomarker EGFR-TK 4-anilino-quinazoline |
| 基金项目:：国家自然科学基金重点项目（81130028）；黑龙江省科技攻关重大项目（GA12C302）;
国家自然科学基金青年项目（81101088）；
国家自然科学基金青年项目（81101085）；中国博士后科学基金资助项目（2012M510095）；黑龙江省博士后基金资助项目（LBH-Z12199）；
哈尔滨医科大学伍连德青年科学基金（WLD-QN1119） |
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| 中文摘要: |
| 分子成像可在活体状态下直观判断分子靶向药物靶位点存在状态，分子靶向药物与靶位点结合率及精确监测分子靶向药物
的治疗疗效，为临床治疗方案的选择和调整提供依据。EGFR 是多种恶性肿瘤的关键靶点。研究表明放射性核素标记的表皮生长
因子酪氨酸激酶抑制剂是很有潜力的成像探针，其中尤以4-苯氨基-喹唑啉类研究最为广泛。本文简要介绍4-苯氨基- 喹唑啉
不同衍生物的结构及性质。阐述了18F标记4-苯氨基-喹唑啉类的主要方法：先用18F 标记苯氨基，然后将18F标记化合物与喹唑
啉或衍生物进行连接，和18F标记喹唑啉或其衍生物，然后与苯胺或其衍生物进行连接。并且进一步比较不同示踪剂在体外、动物
和人体内生物分布、肿瘤摄取和代谢的异同。特别是对18F标记示踪剂与11C标记示踪剂在动物和人体分布进行比较。尤其是[18F]
ML04肝脏摄取低，肿瘤-本底高，多数学者认为[18F]ML04 是最有潜力成为18F标记表皮生长因子受体酪氨酸激酶抑制剂4- 苯氨
基-喹唑啉类示踪剂。 |
| 英文摘要: |
| Molecular imaging can visually judge the existing state of molecular target site, binding rates of molecular targeted
drugs and target site, and precisely monitor the efficiency of molecular targeted therapy in vivo. It can help to make clinical treatment
options and provide the basis for adjustment. EGFR is a key target for a variety of malignant tumors. Studies have shown that radionuclide-
labeled epidermal growth factor tyrosine kinase inhibitors are promising imaging probes, especially 4-anilino-quinazoline is most
widely studied. This article briefly introduce different structures and properties of 4-anilino-quinazoline derivatives. There are two main
methods labled 4-anilino quinazoline by 18F. Labling phenylamino by 18F, and connected the 18F labeled compound with quinazoline or
quinazoline derivatives. The other one is Labling quinazoline or quinazoline derivatives by18F, and connected the 18F labeled com- pound
with phenylamino. And we compare different tracers' biodistribution, trace uptake and excretion , in animals and human body.
Especially, the distributions of 18F labeled tracers and 11C labeled tracers in animal and human are compared. As 18F labled ML04 has
low liver accumulation and high tumor-backgroud ratio, most researchers believe that the [18F] ML04 is the most potential 18F labeled
tracer of EGFR-TK inhibitor of 4- anilinoquinazoline. |
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