Circular Bivalent Aptamers Enable in Vivo Stability and Recognition,Journal of the American Chemical Society

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Circular Bivalent Aptamers Enable in Vivo Stability and Recognition
Journal of the American Chemical Society ( IF 14.4 ) Pub Date : 2017-06-29 , DOI: 10.1021/jacs.7b04547
Hailan Kuai ₁ , Zilong Zhao ₁ , Liuting Mo ₁ , Hui Liu ₁ , Xiaoxiao Hu ₁ , Ting Fu ₁ , Xiaobing Zhang ₁ , Weihong Tan _{1,

2}

Affiliation

Aptamers are powerful candidates for molecular imaging and targeted therapy of cancer based on such appealing features as high binding affinity, high specificity, site-specific modification and rapid tumor penetration. However, aptamers are susceptible to plasma exonucleases in vivo. This seriously affects their in vivo applications. To overcome this key limitation, we herein report the design and development of circular bivalent aptamers. Systematic studies reveal that cyclization of aptamers can improve thermal stability, nuclease resistance and binding affinity. In vivo fluorescence imaging further validates the efficient accumulation and retention of circular bivalent aptamers in tumors compared to "mono-aptamers". Therefore, this study provides a simple and efficient strategy to boost in vivo aptamer applications in cancer diagnosis and therapy.

中文翻译：

圆形二价适体实现体内稳定性和识别

基于高结合亲和力、高特异性、位点特异性修饰和快速肿瘤渗透等吸引人的特征，适体是癌症分子成像和靶向治疗的有力候选者。然而，适体在体内对血浆外切核酸酶敏感。这严重影响了它们的体内应用。为了克服这一关键限制，我们在此报告了圆形二价适体的设计和开发。系统研究表明，适配体的环化可以提高热稳定性、核酸酶抗性和结合亲和力。与“单适配子”相比，体内荧光成像进一步验证了圆形二价适配子在肿瘤中的有效积累和保留。所以，

更新日期：2017-06-29

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