Manicardi Alex, Gambari Roberto, de Cola Luisa, Corradini Roberto
Department of Chemistry, Life Sciences and Environmental Sustainability, University of Parma, Parma, Italy.
Department of Life Sciences and Biotechnology, University of Ferrara, Ferrara, Italy.
Methods Mol Biol. 2018;1811:49-63. doi: 10.1007/978-1-4939-8582-1_4.
Peptide Nucleic Acids (PNAs) are oligonucleotide mimics that can be used to block the biological action of microRNA, thus affecting gene expression post-transcriptionally. PNAs are obtained with solid-phase peptide synthesis, and can be easily conjugated to other peptides. Conjugation with R8-Peptide or modification of the PNA backbone (at C5 or C2 carbon) with arginine side chains allows efficient cellular uptake. The present protocol describes the synthesis of cationic PNAs that can be used alone as drugs or for efficient co-delivery in suitable inorganic nanocarriers.
肽核酸（PNA）是一种寡核苷酸类似物，可用于阻断微小RNA的生物学作用，从而在转录后影响基因表达。PNA通过固相肽合成获得，并且可以很容易地与其他肽偶联。与R8肽偶联或用精氨酸侧链修饰PNA主链（在C5或C2碳处）可实现高效的细胞摄取。本方案描述了阳离子PNA的合成，其可单独用作药物或用于在合适的无机纳米载体中进行高效共递送。
