Department of Chemistry, Binghamton University, The State University of New York, Binghamton, New York 13902, United States.
ACS Chem Biol. 2013 Aug 16;8(8):1683-6. doi: 10.1021/cb400144x. Epub 2013 Jun 12.
Conjugation of short peptide nucleic acids (PNA) with tetralysine peptides strongly enhanced triple helical binding to RNA at physiologically relevant conditions. The PNA hexamers and heptamers carrying cationic nucleobase and tetralysine modifications displayed high binding affinity for complementary double-stranded RNA without compromising sequence selectivity. The PNA-peptide conjugates had unique preference for binding double-stranded RNA, while having little, if any, affinity for double-stranded DNA. The cationic PNAs were efficiently taken up by HEK293 cells, whereas little uptake was observed for unmodified PNA.
短肽核酸 (PNA) 与四赖氨酸肽的缀合强烈增强了在生理相关条件下与 RNA 的三螺旋结合。携带阳离子碱基和四赖氨酸修饰的 PNA 六聚体和七聚体对互补双链 RNA 具有高结合亲和力,而不影响序列选择性。PNA-肽缀合物对双链 RNA 具有独特的结合偏好,而对双链 DNA 的亲和力很小,如果有的话。阳离子 PNAs 被 HEK293 细胞有效摄取,而未修饰的 PNA 摄取很少。