首页> 外国专利> OLIGO-GUANIDINES BASED CELLULAR TRANSPORTER FOR EFFECTIVE DELIVERY OF NONPENETRABLE CARGOS IN-VITRO AND IN-VIVO

OLIGO-GUANIDINES BASED CELLULAR TRANSPORTER FOR EFFECTIVE DELIVERY OF NONPENETRABLE CARGOS IN-VITRO AND IN-VIVO

机译:基于寡聚寡核苷酸的细胞转运蛋白,可有效递送体内和体外不可穿透的货物

摘要

Oligo-guanidines based cellular transporter are provided comprising heterocyclic rings including 4-aminopiperidine, piperazine, morpholine having at least one N-terminal based heterocyclic ring or at least one O-heteroatom based heterocyclic ring tailored with hydrophobic and/or lipophilic group and related compounds adapted as cell penetrating agents/ carriers, and also relates to its method of preparation. Said oligo-guanidines are adapted as effective molecular transporters for transport and/or delivery of therapeutics, therapeutic candidates, probes, or other molecules of interest across biological barriers including oligonucleotides. Advantageously, said oligo- guanidines are capable of being internalized into cells (in-vitro and in-vivo) with enhanced cellular uptake in nanomolar concentration.
机译:提供了基于寡胍的细胞转运蛋白,其包含杂环,所述杂环包括4-氨基哌啶,哌嗪,具有至少一个基于疏水和/或亲脂性基团的N-末端杂环或至少一个O-杂原子的杂环的吗啉和相关化合物用作细胞穿透剂/载体的化合物,还涉及其制备方法。所述寡胍适于作为有效的分子转运蛋白,用于跨生物屏障(包括寡核苷酸)转运和/或递送治疗剂,候选治疗剂,探针或其他目的分子。有利地,所述寡胍能够以纳摩尔浓度增加细胞摄取而被内在化进入细胞(体外和体内)。

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