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Evaluation of a Tc-99m-labeled cyclic RGD tetramer for noninvasive imaging integrin alpha(v)beta(3)-positive breast cancer
Liu, Shuang1; Hsieh, Wen-Yuan1; Jiang, Young1; Kim, Young-Seung1; Sreerama, Subramanya G.1; Chen, Xiaoyuan1; Jia, Bing1; Wang, Fan1
刊名BIOCONJUGATE CHEMISTRY
2007-03-01
DOI10.1021/bc0603081
18期:2页:438-446
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemical Research Methods ; Biochemistry & Molecular Biology ; Chemistry, Multidisciplinary ; Chemistry, Organic
研究领域[WOS]Biochemistry & Molecular Biology ; Chemistry
关键词[WOS]GLIOMA INTEGRIN-ALPHA(V)BETA(3) EXPRESSION ; TUMOR ANGIOGENESIS ; PEPTIDES ; RADIOPHARMACEUTICALS ; ALPHA-V-BETA-3 ; AGENTS ; CELLS ; DIMER ; LUNG
英文摘要

Integrin alpha(v)beta(3) plays a critical role in tumor angiogenesis and metastasis. Radiolabeled RGD peptides that are integrin alpha(v)beta(3)-specific are very useful for noninvasive imaging of integrin expression in rapidly growing and metastatic tumors. In this study, we determined the binding affinity of E{E[c(RGDfK)](2)}(2) (tetramer) and its 6-hydrazinonicotinamide conjugate (HYNIC-tetramer) against the binding of I-125-echistatin to the integrin alpha(v)beta(3)-positive MDA-MB-435 breast cancer cells. The athymic nude mice bearing MDA-MB-435 xenografts were used to evaluate the potential of ternary ligand complex [Tc-99m(HYNIC-tetramer)(tricine)(TPPTS)] (TPPTS = trisodium triphenylphosphine-3,3′,3′ ′-trisulfonate) as a new radiotracer for imaging breast cancer integrin alpha(v)beta(3) expression by single photon emission computed tomography (SPECT). It was found that the binding affinity of tetramer (IC50 = 51 +/- 11 nM) was slightly higher than that of its dimeric analogue (IC50 = 78 +/- 27 nM) and is comparable to that of the HYNIC-tetramer conjugate (IC50 = 55 +/- 11 nM) within the experimental error. Biodistribution data showed that [Tc-99m(HYNIC-tetramer)(tricine)(TPPTS)] had a rapid blood clearance (4.61 +/- 0.81 %ID/g at 5 min postinjection (p.i.) and 0.56 +/- 0.12 %ID/g at 120 min p.i.) and was excreted mainly via the renal route. [Tc-99m(HYNIC-tetramer)(tricine)(TPPTS)] had high tumor uptake with a long tumor retention (5.60 +/- 0.87 %ID/g and 7.30 +/- 1.32 %ID/g at 5 and 120 min p.i., respectively). The integrin alpha(v)beta(3)-specificity was demonstrated by co-injection of excess E[c(RGDfK)](2), which resulted in a significant reduction in tumor uptake of the radiotracer. The metabolic stability of [Tc-99m(HYNIC-tetramer)(tricine)(TPPTS)] was determined by analyzing urine and feces samples from the tumor-bearing mice at 120 min p.i. In the urine, about 20% of [Tc-99m(HYNIC-tetramer)(tricine)(TPPTS)] remained intact while only similar to 15% metabolized species was detected in feces. SPECT images displayed significant radiotracer localization in tumor with good contrast as early as 1 h p.i. The high tumor uptake and fast renal excretion make [Tc-99m(HYNIC-tetramer)(tricine)(TPPTS)] a promising radiotracer for noninvasive imaging of the integrin alpha(v)beta(3)-positive tumors by SPECT.

语种英语
WOS记录号WOS:000245041500022
引用统计
被引频次:115[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/52821
专题北京大学医药卫生分析中心
作者单位1.Purdue Univ, Sch Hlth Sci, W Lafayette, IN 47907 USA
2.Stanford Univ, Dept Radiol & BioX, Mol Imaging Program Stanford, Stanford, CA 94305 USA
3.Peking Univ, Med Isotopes Res Ctr, Beijing 100083, Peoples R China
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GB/T 7714
Liu, Shuang,Hsieh, Wen-Yuan,Jiang, Young,et al. Evaluation of a Tc-99m-labeled cyclic RGD tetramer for noninvasive imaging integrin alpha(v)beta(3)-positive breast cancer[J]. BIOCONJUGATE CHEMISTRY,2007,18(2):438-446.
APA Liu, Shuang.,Hsieh, Wen-Yuan.,Jiang, Young.,Kim, Young-Seung.,Sreerama, Subramanya G..,...&Wang, Fan.(2007).Evaluation of a Tc-99m-labeled cyclic RGD tetramer for noninvasive imaging integrin alpha(v)beta(3)-positive breast cancer.BIOCONJUGATE CHEMISTRY,18(2),438-446.
MLA Liu, Shuang,et al."Evaluation of a Tc-99m-labeled cyclic RGD tetramer for noninvasive imaging integrin alpha(v)beta(3)-positive breast cancer".BIOCONJUGATE CHEMISTRY 18.2(2007):438-446.
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