ArticleBioorganic & medicinal chemistry2014
Synthesis, [¹⁸F] radiolabeling, and evaluation of poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors for in vivo imaging of PARP-1 using positron emission tomography.
Article in Bioorganic & medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 46 papers.
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Who cites it
46 citing papers in PubMed, 87 citations in OpenAlex.
- Baseline PARP-1 PET imaging in patients with advanced solid tumors with DNA damage response mutations.European journal of nuclear medicine and molecular imaging · 2026Article
- Emerging Radiopharmaceuticals Beyond FDG for Ovarian Cancer: A Review of Advances in Nuclear Medicine.Cancer medicine · 2025Review
- Exploring the radiochemistry of PARP inhibitors: a new era in therapy and imaging.EJNMMI radiopharmacy and chemistry · 2025Review
- PARP1-targeted alpha therapy enhances target expression.EJNMMI research · 2025Article
- Preclinical evaluation of the potential PARP-imaging probe [carbonyl-EJNMMI radiopharmacy and chemistry · 2025Article
- Novel Molecular Classification of Breast Cancer with PET Imaging.Medicina (Kaunas, Lithuania) · 2024Review
- Kinetic Analysis and Metabolism of Poly(Adenosine Diphosphate-Ribose) Polymerase-1-TargetedJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2024Article
- Pharmacodynamic Activity of [JCO precision oncology · 2024Article
- [Journal of clinical medicine · 2024Review
- Effects of combined use of ribociclib with PARP1 inhibitor on cell kinetics in breast cancer.Oncology letters · 2024Article
- Poly(ADP-ribose) polymerase (PARP)-targeted PET imaging in non-oncology application: a pilot study in preclinical models of nonalcoholic steatohepatitis.American journal of nuclear medicine and molecular imaging · 2024Article
- [Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2023Article
- Preclinical evaluation of a brain penetrant PARP PET imaging probe in rat glioblastoma and nonhuman primates.European journal of nuclear medicine and molecular imaging · 2023Article
- [18F]FluorThanatrace ([18F]FTT) PET Imaging of PARP-Inhibitor Drug-Target Engagement as a Biomarker of Response in Ovarian Cancer, a Pilot Study.Clinical cancer research : an official journal of the American Association for Cancer Research · 2023Article
- Preclinical Efficacy of a PARP-1 Targeted Auger-Emitting Radionuclide in Prostate Cancer.International journal of molecular sciences · 2023Article
- Pilot Study: PARP1 Imaging in Advanced Prostate Cancer.Molecular imaging and biology · 2022Article
- Pre-clinical investigation of astatine-211-parthanatine for high-risk neuroblastoma.Communications biology · 2022Article
- [Scientific reports · 2022Article
- Highlight selection of radiochemistry and radiopharmacy developments by editorial board.EJNMMI radiopharmacy and chemistry · 2022Review
- Perspective on the Use of DNA Repair Inhibitors as a Tool for Imaging and Radionuclide Therapy of Glioblastoma.Cancers · 2022Review
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
Abstract
Imaging of poly (ADP-ribose) polymerase-1 (PARP-1) expression in vivo is a potentially powerful tool for developing PARP-1 inhibitors for drug discovery and patient care. We have synthesized several derivatives of benzimidazole carboxamide as PARP-1 inhibitors, which can be (18)F-labeled easily for positron emission tomographic (PET) imaging. Of the compounds synthesized, 12 had the highest inhibition potency for PARP-1 (IC50=6.3 nM). [(18)F]12 was synthesized under conventional conditions in high specific activity with 40-50% decay-corrected yield. MicroPET studies using [(18)F]12 in MDA-MB-436 tumor-bearing mice demonstrated accumulation of [(18)F]12 in the tumor that was blocked by olaparib, suggesting that the uptake of [(18)F]12 in the tumor is specific to PARP-1 expression.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.