Phosphatidylserine targeting for diagnosis and treatment of human diseases.
Phosphatidylserine targeting for diagnosis and treatment of human diseases.
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DOI：
10.1007/s10495-010-0503-y
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发表时间：
2010-09
期刊：
影响因子：
7.2
通讯作者：
Reutelingsperger, Chris
中科院分区：
文献类型：
--
作者：
Schutters, Kristof;Reutelingsperger, Chris
细胞能够通过激活一系列特定的生化反应来执行凋亡。细胞死亡的最显著特征之一是磷脂酰丝氨酸（PS）的外化，其在健康细胞中主要存在于质膜的内小叶中。这些特征使得PS外化成为一种用于诊断目的的成像细胞死亡的充分探索的现象。此外，研究表明，在某些条件下，活细胞在其表面表达PS，如肿瘤血管内皮细胞、应激肿瘤细胞和缺氧心肌细胞。因此，PS已成为针对靶向药物递送的治疗策略的潜在靶点。在这篇综述中，我们强调的生物标志物PS和各种PS结合的化合物，已被用于靶向PS的诊断目的。我们强调35 kD的人蛋白膜联蛋白A5，已被开发为分子成像剂，以测量细胞死亡在体外，和非侵入性体内动物模型和心血管疾病和癌症患者。最近的焦点已经从诊断转移到治疗应用中，采用膜联蛋白A5的策略将药物递送到在其表面表达PS的细胞。
Cells are able to execute apoptosis by activating series of specific biochemical reactions. One of the most prominent characteristics of cell death is the externalization of phosphatidylserine (PS), which in healthy cells resides predominantly in the inner leaflet of the plasma membrane. These features have made PS-externalization a well-explored phenomenon to image cell death for diagnostic purposes. In addition, it was demonstrated that under certain conditions viable cells express PS at their surface such as endothelial cells of tumor blood vessels, stressed tumor cells and hypoxic cardiomyocytes. Hence, PS has become a potential target for therapeutic strategies aiming at Targeted Drug Delivery. In this review we highlight the biomarker PS and various PS-binding compounds that have been employed to target PS for diagnostic purposes. We emphasize the 35 kD human protein annexin A5, that has been developed as a Molecular Imaging agent to measure cell death in vitro, and non-invasively in vivo in animal models and in patients with cardiovascular diseases and cancer. Recently focus has shifted from diagnostic towards therapeutic applications employing annexin A5 in strategies to deliver drugs to cells that express PS at their surface.
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影响因子：
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作者：
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