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A Novel Estrogen Receptor α-Targeted Near-Infrared Fluorescent Probe for in Vivo Detection of Breast Tumor
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2018-09-04 00:00:00 , DOI: 10.1021/acs.molpharmaceut.8b00684 Chu Tang 1, 2 , Yang Du 2, 3, 4 , Qian Liang 2 , Zhen Cheng 5 , Jie Tian 1, 2, 3, 4
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2018-09-04 00:00:00 , DOI: 10.1021/acs.molpharmaceut.8b00684 Chu Tang 1, 2 , Yang Du 2, 3, 4 , Qian Liang 2 , Zhen Cheng 5 , Jie Tian 1, 2, 3, 4
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The ability to detect breast cancer early in its progression is essential to improve patient survival and quality of life. The noninvasive and dynamic imaging and functional assessments of estrogen receptor-alpha (ERα), which is commonly expressed at high levels in breast cancer, are important for effective diagnosis and treatment. Hence, the development of a specific ERα-targeted probe is a major research goal. To that end, in the present study, we created a novel near-infrared (NIR) fluorescent probe, IRDye800CW–E2, for targeted ERα imaging in breast-tumor-bearing mice. IRDye800CW–E2 consisted of a cyanine dye IRDye800CW as the NIR fluorophore and the E2 analogue ethinyl estradiol amine as an ERα targeting ligand. The ethinyl estradiol amine was initially labeled with fluorescein isothiocyanate (FITC) to evaluate the binding specificity to human breast-tumor cells in vitro. Flow chamber and in vitro confocal laser endomicroscopy imaging experiments demonstrated that FITC–E2 was specifically taken up by MCF-7 cells. Furthermore, NIR fluorescence imaging revealed the ability of IRDye800CW–E2 to rapidly target tumors and to achieve good contrast between tumors and background signal 4–48 h postinjection. The fluorescent signal of IRDye800CW–E2 in tumors was successfully blocked by the coinjection of the endogenous ERα-ligand 17β-estradiol (E2) and the probe. Ex vivo fluorescent imaging further confirmed high uptake of the probe by tumors. These results indicated that IRDye800CW–E2 has great potential as an ERα-targeted imaging probe for early breast-tumor detection and has potential for clinical translation.
中文翻译：
体内检测乳腺癌的新型雌激素受体α靶向近红外荧光探针。
早期发现乳腺癌的能力对于提高患者的生存率和生活质量至关重要。雌激素受体-α（ERα）的无创动态成像和功能评估通常在乳腺癌中高水平表达，对有效诊断和治疗很重要。因此，开发特定于ERα的探针是一个主要的研究目标。为此，在本研究中，我们创建了一种新型的近红外（NIR）荧光探针IRDye800CW–E 2，用于荷瘤小鼠中的靶向ERα成像。IRDye800CW–E 2由作为NIR荧光团的花菁染料IRDye800CW和E 2组成类似的乙炔基雌二醇胺作为ERα靶向配体。乙炔雌二醇胺最初用异硫氰酸荧光素（FITC）标记，以评估在体外对人乳腺肿瘤细胞的结合特异性。流动室和体外共聚焦激光内窥镜成像实验表明，FITC–E 2被MCF-7细胞特异性摄取。此外，近红外荧光成像显示IRDye800CW-E 2能够快速靶向肿瘤，并在注射后4–48 h达到肿瘤与背景信号之间的良好对比。IRDye800CW-E的荧光信号2在肿瘤中被成功阻断内源性ERα配体17β雌二醇的共注射（E 2）和探针。离体荧光成像进一步证实了肿瘤对探针的高摄取。这些结果表明，IRDye800CW-E 2作为一种针对ERα的成像探针，对于早期乳腺肿瘤的检测具有巨大的潜力，并具有临床翻译的潜力。
更新日期：2018-09-04
中文翻译：
体内检测乳腺癌的新型雌激素受体α靶向近红外荧光探针。
早期发现乳腺癌的能力对于提高患者的生存率和生活质量至关重要。雌激素受体-α（ERα）的无创动态成像和功能评估通常在乳腺癌中高水平表达，对有效诊断和治疗很重要。因此，开发特定于ERα的探针是一个主要的研究目标。为此，在本研究中，我们创建了一种新型的近红外（NIR）荧光探针IRDye800CW–E 2，用于荷瘤小鼠中的靶向ERα成像。IRDye800CW–E 2由作为NIR荧光团的花菁染料IRDye800CW和E 2组成类似的乙炔基雌二醇胺作为ERα靶向配体。乙炔雌二醇胺最初用异硫氰酸荧光素（FITC）标记，以评估在体外对人乳腺肿瘤细胞的结合特异性。流动室和体外共聚焦激光内窥镜成像实验表明，FITC–E 2被MCF-7细胞特异性摄取。此外，近红外荧光成像显示IRDye800CW-E 2能够快速靶向肿瘤，并在注射后4–48 h达到肿瘤与背景信号之间的良好对比。IRDye800CW-E的荧光信号2在肿瘤中被成功阻断内源性ERα配体17β雌二醇的共注射（E 2）和探针。离体荧光成像进一步证实了肿瘤对探针的高摄取。这些结果表明，IRDye800CW-E 2作为一种针对ERα的成像探针，对于早期乳腺肿瘤的检测具有巨大的潜力，并具有临床翻译的潜力。
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