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N-(2-羟丙基)甲基丙烯酰胺共聚物的胞饮摄取与细胞内降解。一种潜在的药物递送系统。

Pinocytic uptake and intracellular degradation of N-(2-hydroxypropyl)methacrylamide copolymers. A potential drug delivery system.

作者信息

Duncan R, Rejmanova P, Kopecek J, Lloyd J B

出版信息

Biochim Biophys Acta. 1981 Nov 18;678(1):143-50. doi: 10.1016/0304-4165(81)90058-1.

DOI:10.1016/0304-4165(81)90058-1
PMID:7306576
Abstract

Synthetic 125I-labelled N-(2-hydroxypropyl)methacrylamide copolymers containing four different, potentially degradable peptidyl side chains were incubated with rat visceral yolk sacs cultured in vitro. All copolymers were captured by fluid-phase pinocytosis and three of the side chains were susceptible to lysosomal hydrolysis, resulting in release of [125I]iodotyrosine back into the culture medium. Uptake and degradation was completely inhibited by 2,4-dinitrophenol. The thiol-proteinase inhibitor leupeptin did not affect the rate of pinocytosis, but caused different degrees of inhibition of hydrolysis depending on side chain composition.

摘要

将含有四种不同的、潜在可降解肽基侧链的合成125I标记的N-(2-羟丙基)甲基丙烯酰胺共聚物与体外培养的大鼠内脏卵黄囊一起孵育。所有共聚物都通过液相胞饮作用被摄取,并且其中三条侧链易于被溶酶体水解,导致[125I]碘酪氨酸释放回培养基中。2,4-二硝基苯酚完全抑制摄取和降解。巯基蛋白酶抑制剂亮抑酶肽不影响胞饮作用速率,但根据侧链组成会引起不同程度的水解抑制。

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