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

doi:10.1016/j.bmc.2022.116810

	Optimization of ODAP-Urea-based dual-modality PSMA targeting probes for sequential PET-CT and optical imaging
	Li, Yuan 1,2; Duan, Xiaojiang 2,3; Xu, Hongchuang 2; Zhang, Jingming 2; Zhou, Haoxi 4; Zhang, Xiaojun 4; Zhang, Jinming 4; Yang, Zhi 3,5; Hu, Zhenhua6 ; Zhang, Ning 7; Tian, Jie 6,8,9; Yang, Xing 1,2,3
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	被引频次：1[WOS] [WOS记录] [WOS相关记录]
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.