Journal of the American Chemical Society
Journal of the American Chemical Society
5 years ago

Circular Bivalent Aptamers Enable in Vivo Stability and Recognition

Circular Bivalent Aptamers Enable in Vivo Stability and Recognition
Ting Fu, Hailan Kuai, Weihong Tan, Xiaoxiao Hu, Hui Liu, Zilong Zhao, Xiaobing Zhang, Liuting Mo
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.

Publisher URL: http://dx.doi.org/10.1021/jacs.7b04547

DOI: 10.1021/jacs.7b04547

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