CASIA OpenIR  > 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, 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
Source PublicationBIOORGANIC & MEDICINAL CHEMISTRY
ISSN0968-0896
2022-07-15
Volume66Pages:10
Corresponding AuthorTian, Jie(jie.tian@ia.ac.cn) ; Yang, Xing(yangxing2017@bjmu.edu.cn)
AbstractProstate-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.
KeywordProstate cancer Prostate-specific membrane antigen (PSMA) Dual-modality imaging PET imaging Optical imaging
DOI10.1016/j.bmc.2022.116810
WOS KeywordPOSITIVE SURGICAL MARGINS ; PROSTATE-CANCER ; RADICAL PROSTATECTOMY ; BIOLOGICAL EVALUATION ; INHIBITOR ; SURGERY ; AGENTS ; MODEL
Indexed BySCI
Language英语
Funding ProjectNational Natural Science Foundation of China[92059101] ; National Natural Science Foundation of China[21877004] ; National Natural Science Foundation of China[22106006]
Funding OrganizationNational Natural Science Foundation of China
WOS Research AreaBiochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
WOS SubjectBiochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
WOS IDWOS:000802657100002
PublisherPERGAMON-ELSEVIER SCIENCE LTD
Citation statistics
Document Type期刊论文
Identifierhttp://ir.ia.ac.cn/handle/173211/49615
Collection中国科学院分子影像重点实验室
Corresponding AuthorTian, Jie; Yang, Xing
Affiliation1.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
Corresponding Author AffilicationInstitute of Automation, Chinese Academy of Sciences
Recommended Citation
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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