靶向酸性病变组织：基于pH（低）插入肽（pHLIP）应用的新技术。
Targeting acidic diseased tissue: New technology based on use of the pH (Low) Insertion Peptide (pHLIP).
作者信息
Andreev Oleg A, Engelman Donald M, Reshetnyak Yana K
出版信息
Chim Oggi. 2009 Mar 1;27(2):34-37.
Abstract
We discuss a peptide that targets cells in the acidic tissues that result from a range of pathological states, including tumours, and that can also translocate cell-impermeable cargo molecules across cell membranes in a pH-dependent manner. The technology is based on the interactions of a water-soluble membrane peptide, which we call pHLIP (pH (Low) Insertion Peptide), with the lipid bilayers of cell membranes. at the normal pH of healthy tissue it binds to cell surfaces, but at low pH pHLIP inserts as a monomer across the cell membrane to form a stable transmembrane helix. pHLIP holds promise for imaging and drug delivery applications.
摘要
我们讨论了一种肽，它靶向一系列病理状态（包括肿瘤）所导致的酸性组织中的细胞，并且还能以pH依赖的方式将细胞不可渗透的货物分子转运穿过细胞膜。该技术基于一种水溶性膜肽（我们称之为pHLIP，即pH（低）插入肽）与细胞膜脂质双层的相互作用。在健康组织的正常pH值下，它与细胞表面结合，但在低pH值时，pHLIP作为单体插入细胞膜形成稳定的跨膜螺旋。pHLIP在成像和药物递送应用方面具有前景。
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