Controlling the intracellular localization of fluorescent polyamide analogues in cultured cells

被引：47

作者：

Crowley, KS ^{[1
]}

Phillion, DP ^{[1
]}

Woodard, SS ^{[1
]}

Schweitzer, BA ^{[1
]}

Singh, M ^{[1
]}

Shabany, H ^{[1
]}

Burnette, B ^{[1
]}

Hippenmeyer, P ^{[1
]}

Heitmeier, M ^{[1
]}

Bashkin, JK ^{[1
]}

机构：

[1] Pharmacia Corp, St Louis, MO 63198 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 09期

关键词：

D O I：

10.1016/S0960-894X(03)00152-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The intracellular distribution of fluorescent-labeled polyamides was examined in live cells. We showed that BODIPY-labeled polyamides accumulate in acidic vesicles, mainly lysosomes, in the cytoplasm of HCT116 colon cancer cells and human rheumatoid synovial fibroblasts (RSF). Verapamil blocked vesicular accumulation and led to nuclear accumulation of the BODIPY-labeled polyamide in RSFs. We infer that the basic amine group commonly found at the end of synthetic polyamide chains is responsible for their accumulation in cytoplasmic vesicles in mammalian cells. Modifying the charge on a polyamide by replacing the BODIPY moiety with a fluorescein moiety on the amine tail allowed the polyamide to localize in the nucleus of the cell and bypass the cytoplasmic vesicles in HCT116 cells. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：1565 / 1570

页数：6

共 15 条

[1] Solid phase synthesis of polyamides containing imidazole and pyrrole amino acids [J].