Phosphatidylserine targeting for diagnosis and treatment of human diseases

Kristof Schutters*, Chris P. M. Reutelingsperger

*Corresponding author for this work

Research output: Contribution to journalArticleAcademicpeer-review

130 Citations (Web of Science)

Abstract

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.
Original languageEnglish
Pages (from-to)1072-1082
JournalApoptosis
Volume15
Issue number9
DOIs
Publication statusPublished - Sep 2010

Keywords

  • Apoptosis
  • Phosphatidylserine
  • Annexin A5
  • Molecular Imaging
  • Targeted Drug Delivery

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