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An NIR-II Probe with High PSMA Affinity Demonstrates an Unexpected Excellent Bone Imaging Ability

文献类型：期刊论文

作者Zhang, Longfei1; Shi, Xiaojing2; Li, Yuying1; Duan, Xiaojiang3; Yang, Xing3; Hu, Zhenhua2,4; Cui, Mengchao1
刊名JOURNAL OF MEDICINAL CHEMISTRY
出版日期2023-11-16
卷号66期号:23页码:16441-16454
ISSN号0022-2623
DOI10.1021/acs.jmedchem.3c01895
通讯作者Hu, Zhenhua(zhenhua.hu@ia.ac.cn) ; Cui, Mengchao(cmc@bnu.edu.cn)
英文摘要(S)-3-(Carboxyformamido)-2-(3-(carboxymethyl)-ureido)-propanoic acid (EuK) is a known binder toward the prostate-specific membrane agent (PSMA) with strong affinity, making it a popular choice for prostate cancer medicine development. However, during the probe modification, a new EuK-based PSMA tetramer, Bone-1064, was discovered to have an unexpected and intense uptake in bone, which has not yet been reported in any previous studies yet. After administration, Bone-1064 allowed for high contrast visualization of the bone from surrounding tissues with a signal-to-background ratio of 10.22 at 24 h postinjection. In contrast, the tumor had a blurry contour, and the maximum tumor-to-normal-tissue ratio was only 2.22. Further imaging studies revealed that Bone-1064 binds specifically to hydroxyapatite in bone tissues, instead of PSMA. Overall, Bone-1064 is an excellent bone probe with a unique structure that can be used for NIR-II fluorescence imaging in animal models. Meanwhile, this modification study might also inspire further PSMA probe designations.
WOS关键词DESIGN ; DYE ; PET
资助项目National Natural Science Foundation of China[22022601] ; National Natural Science Foundation of China[U1967221] ; National Natural Science Foundation of China[92059207] ; National Natural Science Foundation of China
WOS研究方向Pharmacology & Pharmacy
语种英语
出版者AMER CHEMICAL SOC
WOS记录号WOS:001141455400001
资助机构National Natural Science Foundation of China ; National Natural Science Foundation of China
源URL[http://ir.ia.ac.cn/handle/173211/54841]  
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Hu, Zhenhua; Cui, Mengchao
作者单位1.Beijing Normal Univ, Coll Chem, Key Lab Radiopharmaceut, Minist Educ, Beijing 100875, Peoples R China
2.Chinese Acad Sci, Inst Automat, CAS Key Lab Mol Imaging, Beijing Key Lab Mol Imaging, Beijing 100190, Peoples R China
3.Peking Univ First Hosp, Dept Nucl Med, Beijing 100034, Peoples R China
4.Univ Chinese Acad Sci, Sch Artificial Intelligence, Beijing 100049, Peoples R China
推荐引用方式
GB/T 7714		 Zhang, Longfei,Shi, Xiaojing,Li, Yuying,et al. An NIR-II Probe with High PSMA Affinity Demonstrates an Unexpected Excellent Bone Imaging Ability[J]. JOURNAL OF MEDICINAL CHEMISTRY,2023,66(23):16441-16454.
APA Zhang, Longfei.,Shi, Xiaojing.,Li, Yuying.,Duan, Xiaojiang.,Yang, Xing.,...&Cui, Mengchao.(2023).An NIR-II Probe with High PSMA Affinity Demonstrates an Unexpected Excellent Bone Imaging Ability.JOURNAL OF MEDICINAL CHEMISTRY,66(23),16441-16454.
MLA Zhang, Longfei,et al."An NIR-II Probe with High PSMA Affinity Demonstrates an Unexpected Excellent Bone Imaging Ability".JOURNAL OF MEDICINAL CHEMISTRY 66.23(2023):16441-16454.

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来源：自动化研究所

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