期刊
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
卷 139, 期 27, 页码 9128-9131出版社
AMER CHEMICAL SOC
DOI: 10.1021/jacs.7b04547
关键词
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资金
- NSFC [NSFC 21221003, NSFC 21327009]
- National Institutes of Health [GM079359]
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 cyclitation 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.
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