Development of 2-aminoisobutyric acid (Aib)-rich cell-penetrating foldamers for efficient siRNA delivery

We have designed and synthesized a set of cell-penetrating foldamers (CPFs), Blocks 1-8, composed of the common amino acids Leu, Arg, and Gly, as well as the helicogenic amino acid 2-aminoisobutyric acid. The findings showed that Block 3 could deliver siRNA into cells without significant cytotoxicit...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Chemical communications (Cambridge, England) England), 2019-07, Vol.55 (54), p.7792-7795
Hauptverfasser:	Misawa, Takashi, Ohoka, Nobumichi, Oba, Makoto, Yamashita, Hiroko, Tanaka, Masakazu, Naito, Mikihiko, Demizu, Yosuke
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Sequence Amino acids Aminoisobutyric Acids - chemistry Cell Line, Tumor Cell-Penetrating Peptides - chemical synthesis Cell-Penetrating Peptides - chemistry Cell-Penetrating Peptides - metabolism Cell-Penetrating Peptides - toxicity Drug Carriers - chemical synthesis Drug Carriers - chemistry Drug Carriers - metabolism Drug Carriers - toxicity Gene Knockdown Techniques Gene Silencing Humans Protein Conformation, alpha-Helical Protein Engineering - methods Proto-Oncogene Proteins p21(ras) - genetics RNA, Small Interfering - administration & dosage RNA, Small Interfering - genetics Toxicity
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	We have designed and synthesized a set of cell-penetrating foldamers (CPFs), Blocks 1-8, composed of the common amino acids Leu, Arg, and Gly, as well as the helicogenic amino acid 2-aminoisobutyric acid. The findings showed that Block 3 could deliver siRNA into cells without significant cytotoxicity. We also demonstrated that Block 3 could be applied to selectively kill the oncogene-driven cancer cells. We have designed and synthesized a set of cell-penetrating foldamers (CPFs), Blocks 1-8, composed of the common amino acids Leu, Arg, and Gly, as well as the helicogenic amino acid 2-aminoisobutyric acid.
ISSN:	1359-7345 1364-548X
DOI:	10.1039/c9cc02203a