Institutional Repository of Chinese Acad Sci, Inst Automat, CAS Key Lab Mol Imaging, Beijing 100190, Peoples R China
Optimization of ODAP-Urea-based dual-modality PSMA targeting probes for sequential PET-CT and optical imaging | |
Li, Yuan1,2; Duan, Xiaojiang2,3; Xu, Hongchuang2; Zhang, Jingming2; Zhou, Haoxi4; Zhang, Xiaojun4; Zhang, Jinming4; Yang, Zhi3,5; Hu, Zhenhua6; Zhang, Ning7; Tian, Jie6,8,9; Yang, Xing1,2,3 | |
发表期刊 | BIOORGANIC & MEDICINAL CHEMISTRY |
ISSN | 0968-0896 |
2022-07-15 | |
卷号 | 66页码:10 |
通讯作者 | Tian, Jie(jie.tian@ia.ac.cn) ; Yang, Xing(yangxing2017@bjmu.edu.cn) |
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. |
关键词 | Prostate cancer Prostate-specific membrane antigen (PSMA) Dual-modality imaging PET imaging Optical imaging |
DOI | 10.1016/j.bmc.2022.116810 |
关键词[WOS] | POSITIVE SURGICAL MARGINS ; PROSTATE-CANCER ; RADICAL PROSTATECTOMY ; BIOLOGICAL EVALUATION ; INHIBITOR ; SURGERY ; AGENTS ; MODEL |
收录类别 | SCI |
语种 | 英语 |
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] |
项目资助者 | National Natural Science Foundation of China |
WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
WOS类目 | Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic |
WOS记录号 | WOS:000802657100002 |
出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
引用统计 | |
文献类型 | 期刊论文 |
条目标识符 | http://ir.ia.ac.cn/handle/173211/49615 |
专题 | 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.Peking Univ Hlth Sci Ctr, Inst Med Technol, Beijing 100191, Peoples R China 2.Peking Univ First Hosp, Dept Nucl Med, Beijing 100034, Peoples R China 3.NMPA Key Lab Res & Evaluat Radiopharmaceut, Beijing 100142, Peoples R China 4.Chinese Peoples Liberat Army Gen Hosp, Dept Nucl Med, First Med Ctr 1, Beijing 100853, 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 Acad Sci, Inst Automat, CAS Key Lab Mol Imaging, State Key Lab Management & Control Complex Syst, Beijing 100190, Peoples R China 7.Peking Univ First Hosp, Translat Canc Res Ctr, Beijing 100034, Peoples R China 8.Xidian Univ, Engn Res Ctr Mol & Neuro Imaging, Sch Life Sci & Technol, Minist Educ, Xi'an 710071, Peoples R China 9.Beihang Univ, Beijing Adv Innovat Ctr Big Data Based Precis Med, Sch Engn Med, Beijing 100191, Peoples R China |
通讯作者单位 | 中国科学院自动化研究所 |
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. |
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