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

doi:10.1021/acs.jmedchem.3c01895

	An NIR-II Probe with High PSMA Affinity Demonstrates an Unexpected Excellent Bone Imaging Ability
	Zhang, Longfei 1; Shi, Xiaojing2 ; Li, Yuying 1; Duan, Xiaojiang 3; Yang, Xing 3; Hu, Zhenhua2,4 ; Cui, Mengchao 1
发表期刊	JOURNAL OF MEDICINAL CHEMISTRY
ISSN	0022-2623
	2023-11-16
卷号	66 期号:23 页码:16441-16454
通讯作者	Hu, Zhenhua(zhenhua.hu@ia.ac.cn) ; Cui, Mengchao(cmc@bnu.edu.cn)
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.
DOI	10.1021/acs.jmedchem.3c01895
关键词[WOS]	DESIGN ; DYE ; PET
收录类别	SCI
语种	英语
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
项目资助者	National Natural Science Foundation of China ; National Natural Science Foundation of China
WOS研究方向	Pharmacology & Pharmacy
WOS类目	Chemistry, Medicinal
WOS记录号	WOS:001141455400001
出版者	AMER CHEMICAL SOC
引用统计
文献类型	期刊论文
条目标识符	http://ir.ia.ac.cn/handle/173211/54842
专题	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
通讯作者单位	中国科学院分子影像重点实验室
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.