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${alpha}$-Amino Acid Pendant Polymers as Endosomal pH-Responsive Gene Carriers
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  • ${alpha}$-Amino Acid Pendant Polymers as Endosomal pH-Responsive Gene Carriers
  • ${alpha}$-Amino Acid Pendant Polymers as Endosomal pH-Responsive Gene Carriers
저자명
Wada. Takuya,Kano. Arihiro,Shimada. Naohiko,Maruyama. Atsushi
간행물명
Macromolecular research
권/호정보
2012년|20권 3호|pp.302-308 (7 pages)
발행정보
한국고분자학회
파일정보
정기간행물|ENG|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

In order to prepare gene carriers responsive to an endosomal pH, amino groups of linear poly(allylamine) (PAA) or poly($L$-lysine) (PLL) were coupled with a-carboxyl groups of ${alpha}$-amino acids (Gly, His, Lys, Arg, and Orn). Acid-base titration indicated that Lys-, Arg-, and Orn-pendant polymers had both strongly basic groups and endosomal pH-responsive ${alpha}$-amino groups. These polymers, like PAA and PLL, formed stable complexes with DNA. Lys-, Arg-, and Orn-pendant polymers were effective transfection reagents independent of the backbone polymers. The pH-responsive ${alpha}$-amino groups enhanced transfection activity as shown by the observation that acetylation of the ${alpha}$-amino group resulted in a considerable loss in transfection activity. These results strongly suggested a lysosomotropic activity of the ${alpha}$-amino groups. Among the ${alpha}$-amino acid-pendant polymers tested, the Orn-pendant polymer exhibited the highest transfection activity/toxicity index. Since PLL with ${alpha}$-amino acid-pendants is composed of naturally occurring amino acids, it is expected to be biodegradable, and these reagents have promise as gene carriers.