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Advancements in PARP1 Targeted Nuclear Imaging and Theranostic Probes
- Source :
- Journal of Clinical Medicine, Vol 9, Iss 2130, p 2130 (2020), Journal of Clinical Medicine
- Publication Year :
- 2020
- Publisher :
- MDPI AG, 2020.
-
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.
- Subjects :
- EXPRESSION
PARP1 tracers
Tailored therapy
Nuclear imaging
Cancer therapy
GLIOBLASTOMA
PARP1 theranostic probes
lcsh:Medicine
Review
Olaparib
PET/SPECT imaging
DELIVERY
03 medical and health sciences
chemistry.chemical_compound
0302 clinical medicine
PARP1
Spect imaging
Medicine
STRATEGY
030304 developmental biology
SPECT imaging
0303 health sciences
business.industry
PARP inhibition
lcsh:R
OLAPARIB
INHIBITOR
Cancer
IN-VITRO
General Medicine
medicine.disease
PET
DNA-DAMAGE
chemistry
030220 oncology & carcinogenesis
PARP inhibitor
Cancer research
RADIOTRACER
Auger and Alpha emitters
business
Subjects
Details
- Language :
- English
- ISSN :
- 20770383
- Volume :
- 9
- Issue :
- 2130
- Database :
- OpenAIRE
- Journal :
- Journal of Clinical Medicine
- Accession number :
- edsair.doi.dedup.....e2751256a8bea242d6eb6976830c37f9