Department of Chemistry, Ball State University, Muncie, IN, USA.
Methods Mol Biol. 2023;2709:105-115. doi: 10.1007/978-1-0716-3417-2_6.
In the field of nucleic acid nanotechnology and therapeutics, there is an imperative need to improve the oligodeoxynucleotides' (ODNs) properties by either chemical modification of the oligonucleotides' structure or to covalently link them to a reporter or therapeutic moieties that possess biologically relevant properties. The chemical conjugation can thus significantly improve the intrinsic properties not only of ODNs but also reporter/therapeutic molecules. Bioconjugation of nucleic acids to small molecules also serves as a nano-delivery facility to transport various functionalities to specific targets. Herein, we describe a generalized methodology that deploys azide-alkyne cycloaddition, a click reaction to conjugate a cyanine-3 alkyne moiety to an azide-functionalized ODN 12-mer, as well as 3-azido 7-hydroxycoumarin to an alkyne functionalized ODN 12-mer.
在核酸纳米技术和治疗学领域，通过化学修饰寡核苷酸的结构或共价连接报告分子或治疗分子，提高寡脱氧核苷酸（ODN）的性质是当务之急。这种化学偶联可以显著改善不仅是 ODN 而且是报告分子/治疗分子的固有性质。核酸与小分子的生物缀合也可用作纳米递药设施，将各种功能输送到特定的靶标。在此，我们描述了一种通用的方法，该方法利用叠氮-炔环加成反应（点击反应）将一个氰基 3 炔基部分连接到一个叠氮功能化的 12 聚体 ODN 上，以及将 3-叠氮基 7-羟基香豆素连接到一个炔基功能化的 12 聚体 ODN 上。
