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Advancements in PARP1 Targeted Nuclear Imaging and Theranostic Probes
Ramya Ambur Sankaranarayanan1, Susanne Kossatz2,3,4, Wolfgang Weber2
1Department of Nuclear Medicine, University Hospital Aachen, RWTH Aachen University, 52074 Aachen, Germany.
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 gBRCAmut 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.
Insights
Novel imaging tracers targeting Poly-(ADP ribose) polymerase 1 (PARP1) show promise for cancer diagnosis and therapy. These tracers can help predict treatment response and deliver targeted therapies, advancing personalized cancer care.
Area of Science:
- Oncology
- Molecular Imaging
- Nuclear Medicine
Background:
- Targeting molecular biomarkers is central to novel cancer therapies.
- Poly-(ADP ribose) polymerase 1 (PARP1) is a key DNA repair enzyme and a validated target in certain cancers.
- PARP1 overexpression in various cancers highlights its potential as both a therapeutic and imaging target.
Purpose of the Study:
- To review advancements in pre-clinical imaging and theranostic PARP1-targeted tracers.
- To explore the diagnostic and therapeutic potential of PARP1-targeted agents.
- To discuss the future of PARP1-targeted theranostics and personalized medicine.
Main Methods:
- Review of recent pre-clinical research on PARP1-targeted tracers.
- Analysis of imaging probes utilizing fluorescent or radionuclide labels.
- Evaluation of tracers that have advanced to clinical trials.
Main Results:
- Several imaging probes targeting PARP1 have been developed, with three currently in clinical evaluation.
- PARP1-targeted tracers demonstrate potential for detecting primary tumors and metastases.
- These tracers can facilitate the targeted delivery of therapeutic radionuclides to tumors overexpressing PARP1.
Conclusions:
- PARP1-targeted imaging tracers offer diagnostic value and can guide personalized therapy.
- The development of theranostic PARP1 inhibitors is advancing nuclear medicine towards tailored cancer treatment.
- PARP1-targeted theranostics represent a promising future for personalized cancer therapy and improved patient prognosis.
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