2. Academic Validation
  3. PARPi-FL--a fluorescent PARP1 inhibitor for glioblastoma imaging

PARPi-FL--a fluorescent PARP1 inhibitor for glioblastoma imaging

  • Neoplasia. 2014 May;16(5):432-40. doi: 10.1016/j.neo.2014.05.005.
Christopher P Irwin 1,  Yasiri Portorreal 1,  Christian Brand 1,  Yachao Zhang 1,  Pooja Desai 1,  Beatriz Salinas 1,  Wolfgang A Weber 2,  Thomas Reiner 3
Affiliations

Affiliations

  • 1 Radiochemistry and Imaging Sciences Service, Department of Radiology, Memorial Sloan Kettering Cancer Center, New York, NY, 10065, USA.
  • 2 Molecular Imaging and Therapy Service, Department of Radiology, Memorial Sloan Kettering Cancer Center, New York, NY, 10065, USA; Molecular Pharmacology and Chemistry Program, Memorial Sloan Kettering Cancer Center, New York, NY, 10065, USA.
  • 3 Radiochemistry and Imaging Sciences Service, Department of Radiology, Memorial Sloan Kettering Cancer Center, New York, NY, 10065, USA; Center for Molecular Imaging and Nanotechnology, Memorial Sloan Kettering Cancer Center, New York, NY, 10065, USA. Electronic address: reinert@mskcc.org.
PMID: 24970386 DOI: 10.1016/j.neo.2014.05.005
Abstract

New intravital optical imaging technologies have revolutionized our understanding of mammalian biology and continue to evolve rapidly. However, there are only a limited number of imaging probes available to date. In this study, we investigated in mouse models of glioblastoma whether a fluorescent small molecule inhibitor of the DNA repair Enzyme PARP1, PARPi-FL, can be used as an imaging agent to detect glioblastomas in vivo. We demonstrated that PARPi-FL has appropriate biophysical properties, low toxicity at concentrations used for imaging, high stability in vivo, and accumulates selectively in glioblastomas due to high PARP1 expression. Importantly, subcutaneous and orthotopic glioblastoma xenografts were imaged with high contrast clearly defining tumor tissue from normal surrounding tissue. This research represents a step toward exploring and developing PARPi-FL as an optical intraoperative imaging agent for PARP1 in the clinic.

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