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Optimization of ODAP-Urea-based dual-modality PSMA targeting probes for sequential PET-CT and optical imaging

文献类型：期刊论文

作者Li, Yuan8,9; Duan, Xiaojiang7,8; Xu, Hongchuang8; Zhang, Jingming8; Zhou, Haoxi6; Zhang, Xiaojun6; Zhang, Jinming6; Yang, Zhi5,7; Hu, Zhenhua4; Zhang, Ning3
刊名BIOORGANIC & MEDICINAL CHEMISTRY
出版日期2022-07-15
卷号66页码:10
ISSN号0968-0896
关键词Prostate cancer Prostate-specific membrane antigen (PSMA) Dual-modality imaging PET imaging Optical imaging
DOI10.1016/j.bmc.2022.116810
通讯作者Tian, Jie(jie.tian@ia.ac.cn) ; Yang, Xing(yangxing2017@bjmu.edu.cn)
英文摘要Prostate-specific membrane antigen (PSMA) is emerging as a promising target to specifically image prostate cancer. Dual-modality probe combining radionuclide imaging and near-infrared fluorescence navigation targeting PSMA would enable both the preoperative staging and intraoperative detection of the tumor lesions. To overcome one of the key barriers for achieving high contrast imaging at both early and late time points, we optimized the pharmacokinetics of dual-modality probes based on oxalyldiaminopropionic acid-urea (ODAPUrea) PSMA inhibitors recently developed. Four dual-modality probes with variable hydrophilicity were synthesized and evaluated. They displayed good optical properties (lambda em max = 835 nm, QY = 0.67%-1.50%), high affinity to PSMA (Ki = 2.09 +/- 1.71-4.15 +/- 2.20 nM) and PSMA specific cellular uptake (0.48 +/- 0.01% - 0.64 +/- 0.04% IA/105 LNCaP cells) upon labeled with 68Ga. In vivo studies showed that [68Ga]Ga-P3 exhibited an optimum pharmacokinetic property with high specific tumor uptake (SUVmax = 1.88 +/- 0.36, at 1 h) in medium level PSMA expressing 22Rv1 tumor model and high tumor-to-muscle ratio (12.56 +/- 2.63, at 1 h). Specific fluorescence imaging could also be achieved with high contrast for later time points (tumor-to-background ratio = 11.63 +/- 4.16 at 24 h). This study demonstrates that ODAP-Urea-based P3 has the potential for PET imaging and intraoperative optical imaging of prostate cancer.
WOS关键词POSITIVE SURGICAL MARGINS ; PROSTATE-CANCER ; RADICAL PROSTATECTOMY ; BIOLOGICAL EVALUATION ; INHIBITOR ; SURGERY ; AGENTS ; MODEL
资助项目National Natural Science Foundation of China[92059101] ; National Natural Science Foundation of China[21877004] ; National Natural Science Foundation of China[22106006]
WOS研究方向Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
语种英语
出版者PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号WOS:000802657100002
资助机构National Natural Science Foundation of China
源URL[http://ir.ia.ac.cn/handle/173211/49614]  
专题自动化研究所_中国科学院分子影像重点实验室
通讯作者Tian, Jie; Yang, Xing
作者单位1.Beihang Univ, Beijing Adv Innovat Ctr Big Data Based Precis Med, Sch Engn Med, Beijing 100191, Peoples R China
2.Xidian Univ, Engn Res Ctr Mol & Neuro Imaging, Sch Life Sci & Technol, Minist Educ, Xi'an 710071, Peoples R China
3.Peking Univ First Hosp, Translat Canc Res Ctr, Beijing 100034, Peoples R China
4.Chinese Acad Sci, Inst Automat, CAS Key Lab Mol Imaging, State Key Lab Management & Control Complex Syst, Beijing 100190, Peoples R China
5.Peking Univ Canc Hosp & Inst, Dept Nucl Med, Key Lab Carcinogenesis & Translat Res, Minist Educ, Beijing 100142, Peoples R China
6.Chinese Peoples Liberat Army Gen Hosp, Dept Nucl Med, First Med Ctr 1, Beijing 100853, Peoples R China
7.NMPA Key Lab Res & Evaluat Radiopharmaceut, Beijing 100142, Peoples R China
8.Peking Univ First Hosp, Dept Nucl Med, Beijing 100034, Peoples R China
9.Peking Univ Hlth Sci Ctr, Inst Med Technol, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714		 Li, Yuan,Duan, Xiaojiang,Xu, Hongchuang,et al. Optimization of ODAP-Urea-based dual-modality PSMA targeting probes for sequential PET-CT and optical imaging[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2022,66:10.
APA Li, Yuan.,Duan, Xiaojiang.,Xu, Hongchuang.,Zhang, Jingming.,Zhou, Haoxi.,...&Yang, Xing.(2022).Optimization of ODAP-Urea-based dual-modality PSMA targeting probes for sequential PET-CT and optical imaging.BIOORGANIC & MEDICINAL CHEMISTRY,66,10.
MLA Li, Yuan,et al."Optimization of ODAP-Urea-based dual-modality PSMA targeting probes for sequential PET-CT and optical imaging".BIOORGANIC & MEDICINAL CHEMISTRY 66(2022):10.

入库方式： OAI收割

来源：自动化研究所

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