环状二价适体赋予体内稳定性和识别能力。
Circular Bivalent Aptamers Enable in Vivo Stability and Recognition.
机构信息
Molecular Science and Biomedicine Laboratory, State Key Laboratory for Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, College of Life Sciences, and Aptamer Engineering Center of Hunan Province, Hunan University , Changsha 410082, China.
Departments of Chemistry, Departments of Physiology and Functional Genomics, Center for Research at the Bio/Nano Interface, UF Health Cancer Center, UF Genetics Institute and McKnight Brain Institute, University of Florida , Gainesville, Florida 32611, United States.
出版信息
J Am Chem Soc. 2017 Jul 12;139(27):9128-9131. doi: 10.1021/jacs.7b04547. Epub 2017 Jun 29.
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.
适体作为一种强大的候选分子，可用于癌症的分子成像和靶向治疗，具有高亲和力、高特异性、特异性修饰和快速肿瘤穿透等诱人特性。然而，适体在体内易受血浆外切核酸酶的影响。这严重影响了它们的体内应用。为了克服这一关键限制，我们在此报告了环状二价适体的设计和开发。系统研究表明，适体的环化可以提高热稳定性、核酸酶抗性和结合亲和力。体内荧光成像进一步验证了与“单适体”相比，环状二价适体在肿瘤中的有效积累和保留。因此，这项研究为提高适体在癌症诊断和治疗中的体内应用提供了一种简单有效的策略。
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