CASIA OpenIR  > 中国科学院分子影像重点实验室
Improved Tumor Targeting and Longer Retention Time of NIR Fluorescent Probes Using Bioorthogonal Chemistry
Zhang, Xianghan1; Wang, Bo1; Zhao, Na1; Tian, Zuhong3; Dai, Yunpeng1; Nie, Yongzhan3; Tian, Jie1,2; Wang, Zhongliang1; Chen, Xiaoyuan4
Source PublicationTHERANOSTICS
AbstractThe traditional labeling method for targeted NIR fluorescence probes requires directly covalent-bonded conjugation of targeting domains and fluorophores in vitro. Although this strategy works well, it is not sufficient for detecting or treating cancers in vivo, due to steric hindrance effects that relatively large fluorophore molecules exert on the configurations and physiological functions of specific targeting domains. The copper-free, "click-chemistry"-assisted assembly of small molecules in living systems may enhance tumor accumulation of fluorescence probes by improving the binding affinities of the targeting factors. Here, we employed a vascular homing peptide, GEBP11, as a targeting factor for gastric tumors, and we demonstrate its effectiveness for in vivo imaging via click-chemistry-mediated conjugation with fluorescence molecules in tumor xenograft mouse models. This strategy showed higher binding affinities than those of the traditional conjugation method, and our results showed that the tumor accumulation of click-chemistry-mediated probes are 11-fold higher than that of directly labeled probes. The tracking life was prolonged by 12-fold, and uptake of the probes into the kidney was reduced by 6.5-fold. For lesion tumors of different sizes, click-chemistry-mediated probes can achieve sufficient signal-to-background ratios (3.5-5) for in vivo detection, and with diagnostic sensitivity approximately 3.5 times that of traditional labeling probes. The click-chemistry-assisted detection strategy utilizes the advantages of "small molecule" probes while not perturbing their physiological functions; this enables tumor detection with high sensitivity and specific selectivity.
KeywordClick Chemistry Nir Fluorescence Probes Gebp11 Gastric Cancer
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine
Indexed BySCI
Funding OrganizationProgram of the National Basic Research and Development Program of China (973)(2013CB733803) ; National Natural Science Foundation of China(81227901 ; national 1000 Young Talents Program of China ; 81402467 ; 81671753)
WOS Research AreaResearch & Experimental Medicine
WOS SubjectMedicine, Research & Experimental
WOS IDWOS:000408444200014
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Cited Times:8[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Affiliation1.Xidian Univ, Engn Res Ctr Mol Imaging & Neuroimaging, Minist Educ, Sch Life Sci & Technol, Xian 710026, Shaanxi, Peoples R China
2.Chinese Acad Sci, Inst Automat, Beijing 100190, Peoples R China
3.Fourth Mil Med Univ, Inst Digest Dis, Xijing Hosp, Xian 710032, Shaanxi, Peoples R China
4.Natl Inst Biomed Imaging & Bioengn, Lab Mol Imaging & Nanomed, NIH, Bethesda, MD 20892 USA
Recommended Citation
GB/T 7714
Zhang, Xianghan,Wang, Bo,Zhao, Na,et al. Improved Tumor Targeting and Longer Retention Time of NIR Fluorescent Probes Using Bioorthogonal Chemistry[J]. THERANOSTICS,2017,7(15):3794-3802.
APA Zhang, Xianghan.,Wang, Bo.,Zhao, Na.,Tian, Zuhong.,Dai, Yunpeng.,...&Chen, Xiaoyuan.(2017).Improved Tumor Targeting and Longer Retention Time of NIR Fluorescent Probes Using Bioorthogonal Chemistry.THERANOSTICS,7(15),3794-3802.
MLA Zhang, Xianghan,et al."Improved Tumor Targeting and Longer Retention Time of NIR Fluorescent Probes Using Bioorthogonal Chemistry".THERANOSTICS 7.15(2017):3794-3802.
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