Cell death is involved in many pathological conditions, and there is a need for clinical imaging agents that can target and report cell death. One the best known biomarkers of cell death is exposure of the anionic phospholipid phosphatidylserine (PS) on the surface of dying cells. There is a need for effective PS-binding probes with high binding affinity and selectivity while maintaining good in vivo properties. Our group has previously shown that small molecule zinc(II)-bis(dipicolylamine) (Zn2BDPA) coordination complexes have promising PS-recognition ability. The present study examines the cell death targeting ability of a modified Zn2BDPA structure with a tyrosine scaffold. Studies using probes with deep-red fluorescent labels show selective PS targeting in vesicles, cell culture, and two in vivo small animal models of cell death. In addition, the probes exhibit favorable biodistribution profiles and thus are promising candidates for additional studies of cell death imaging in living subjects.

Cell death imaging using fluorescent probes for phosphatidylserine

249th National Meeting (2015)

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