Design, Synthesis, and Biological Evaluation of a Small-Molecule PET Agent for Imaging PD-L1 Expression

doi:10.3390/ph16020213

科研成果详情

题名	Design, Synthesis, and Biological Evaluation of a Small-Molecule PET Agent for Imaging PD-L1 Expression
作者	Xu, Liang1,2; Zhang, Lixia1,2; Liang, Beibei1,2; Zhu, Shiyu 2; Lv, Gaochao 2; Qiu, Ling1,2; Lin, Jianguo 1,2
发表日期	2023-02
发表期刊	PHARMACEUTICALS 影响因子和分区
语种	英语
原始文献类型	Article
关键词	PET PD-L1 small-molecule imaging agent tumor
其他关键词	CANCER ; NIVOLUMAB ; DOCETAXEL ; THERAPY
摘要	Immunotherapy blocking programmed cell death protein 1/programmed death ligand 1 (PD-1/PD-L1) pathway has achieved great therapeutic effect in the clinic, but the overall response rate is not satisfactory. Early studies showed that response to treatment and overall survival could be positively related to PD-L1 expression in tumors. Therefore, accurate measurement of PD-L1 expression will help to screen cancer patients and improve the overall response rate. A small molecular positron emission tomography (PET) probe [F-18]LP-F containing a biphenyl moiety was designed and synthesized for measurement of PD-L1 expression in tumors. The PET probe [F-18]LP-F was obtained with a radiochemical yield of 12.72 +/- 1.98%, a radiochemical purity of above 98% and molar activity of 18.8 GBq/mu mol. [F-18]LP-F had good stability in phosphate buffer saline (PBS) and mouse serum. In vitro assay indicated that [F-18]LP-F showed moderate affinity to PD-L1. Micro-PET results showed that the tumor accumulation of [F-18]LP-F in A375 tumor was inferior to that in A375-hPD-L1 tumor. All the results demonstrated that [F-18]LP-F could specifically bind to PD-L1 and had a potential application in non-invasive evaluation of PD-L1 expression in tumors.
资助项目	National Natural Science Foundation of China [81972906]; Natural Science Foundation of Jiangsu Province [BK20201134]; Major Scientific Research Project of Jiangsu Commission of Health [ZDA2020007]; Science Technology and Development Project of Wuxi [Y20212013]
出版者	MDPI
ISSN	1424-8247
EISSN	1424-8247
卷号	16 期号:2
DOI	10.3390/ph16020213
页数	12
WOS类目	Chemistry, Medicinal ; Pharmacology & Pharmacy
WOS研究方向	Pharmacology & Pharmacy
WOS记录号	WOS:000940959300001
收录类别	SCIE ; SCOPUS ; PUBMED
URL	查看原文
PubMed ID	37259361
SCOPUSEID	2-s2.0-85148947918
通讯作者地址	[Qiu, Ling]School of Basic Medical Sciences,Wenzhou Medical University,Wenzhou,325035,China ; [Lin, Jianguo]School of Basic Medical Sciences,Wenzhou Medical University,Wenzhou,325035,China
Scopus学科分类	Molecular Medicine;Pharmaceutical Science;Drug Discovery
引用统计
文献类型	期刊论文
条目标识符	https://kms.wmu.edu.cn/handle/3ETUA0LF/174616
专题	基础医学院（机能实验教学中心）
通讯作者	Qiu, Ling; Lin, Jianguo
作者单位	1.School of Basic Medical Sciences,Wenzhou Medical University,Wenzhou,325035,China; 2.NHC Key Laboratory of Nuclear Medicine,Jiangsu Key Laboratory of Molecular Nuclear Medicine,Jiangsu Institute of Nuclear Medicine,Wuxi,214063,China
第一作者单位	基础医学院（机能实验教学中心）
通讯作者单位	基础医学院（机能实验教学中心）
第一作者的第一单位	基础医学院（机能实验教学中心）
推荐引用方式 GB/T 7714	Xu, Liang,Zhang, Lixia,Liang, Beibei,et al. Design, Synthesis, and Biological Evaluation of a Small-Molecule PET Agent for Imaging PD-L1 Expression[J]. PHARMACEUTICALS,2023,16(2).
APA	Xu, Liang., Zhang, Lixia., Liang, Beibei., Zhu, Shiyu., Lv, Gaochao., ... & Lin, Jianguo. (2023). Design, Synthesis, and Biological Evaluation of a Small-Molecule PET Agent for Imaging PD-L1 Expression. PHARMACEUTICALS, 16(2).
MLA	Xu, Liang,et al."Design, Synthesis, and Biological Evaluation of a Small-Molecule PET Agent for Imaging PD-L1 Expression".PHARMACEUTICALS 16.2(2023).