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

doi:10.1016/j.bmc.2022.116810

CORC > 自动化研究所 > 中国科学院自动化研究所 > 中国科学院分子影像重点实验室

	Optimization of ODAP-Urea-based dual-modality PSMA targeting probes for sequential PET-CT and optical imaging
	Li, Yuan 8,9; Duan, Xiaojiang 7,8; Xu, Hongchuang 8; Zhang, Jingming 8; Zhou, Haoxi 6; Zhang, Xiaojun 6; Zhang, Jinming 6; Yang, Zhi 5,7; Hu, Zhenhua 4; Zhang, Ning 3
刊名	BIOORGANIC & MEDICINAL CHEMISTRY
	2022-07-15
卷号	66 页码:10
关键词	Prostate cancer Prostate-specific membrane antigen (PSMA) Dual-modality imaging PET imaging Optical imaging
ISSN号	0968-0896
DOI	10.1016/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.
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关键词	POSITIVE SURGICAL MARGINS ; PROSTATE-CANCER ; RADICAL PROSTATECTOMY ; BIOLOGICAL EVALUATION ; INHIBITOR ; SURGERY ; AGENTS ; MODEL
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
内容类型	期刊论文
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.