Advancements in PARP1 Targeted Nuclear Imaging and Theranostic Probes

Ramya Ambur Sankaranarayanan, Susanne Kossatz, Wolfgang Weber, Mohsen Beheshti, Agnieszka Morgenroth, Felix M. Mottaghy*

*Corresponding author for this work

Research output: Contribution to journal(Systematic) Review article peer-review

Abstract

The central paradigm of novel therapeutic approaches in cancer therapy is identifying and targeting molecular biomarkers. One such target is the nuclear DNA repair enzyme Poly-(ADP ribose) polymerase 1 (PARP1). Sensitivity to PARP inhibition in certain cancers such as gBRCA(mut)breast and ovarian cancers has led to its exploitation as a target. The overexpression of PARP1 in several types of cancer further evoked interest in its use as an imaging target. While PARP1-targeted inhibitors have fast developed and approved in this past decade, determination of PARP1 expression might help to predict the response to PARP inhibitor treatment. This has the potential of improving prognosis and moving towards tailored therapy options and/or dosages. This review summarizes the recent pre-clinical advancements in imaging and theranostic PARP1 targeted tracers. To assess PARP1 levels, several imaging probes with fluorescent or beta/gamma emitting radionuclides have been proposed and three have advanced to ongoing clinical evaluation. Apart from its diagnostic value in detection of primary tumors as well as metastases, this shall also help in delivering therapeutic radionuclides to PARP1 overexpressing tumors. Henceforth nuclear medicine has now advanced towards conjugating theranostic radionuclides to PARP1 inhibitors. This paves the way for a future of PARP1-targeted theranostics and personalized therapy.

Original languageEnglish
Article number2130
Number of pages15
JournalJournal of Clinical Medicine
Volume9
Issue number7
DOIs
Publication statusPublished - Jul 2020

Keywords

  • PARP inhibition
  • PARP1 tracers
  • PARP1 theranostic probes
  • PET
  • SPECT imaging
  • Auger and Alpha emitters
  • DNA-DAMAGE
  • IN-VITRO
  • EXPRESSION
  • INHIBITOR
  • GLIOBLASTOMA
  • RADIOTRACER
  • STRATEGY
  • OLAPARIB
  • DELIVERY
  • PET/SPECT imaging

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