Initial evaluation of Cu-64 labeled PARPi-DOTA PET imaging in mice with mesothelioma
| Autor: | Jiang He, Anna B. Banizs, Pengcheng Hu, Tao Huang |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
Male
Mesothelioma 0301 basic medicine Biodistribution Clinical Biochemistry Mice Nude Pharmaceutical Science Biochemistry Article Piperazines Olaparib Heterocyclic Compounds 1-Ring Mice 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine In vivo Drug Discovery medicine Animals DOTA Tissue Distribution Molecular Biology medicine.diagnostic_test Organic Chemistry medicine.disease 030104 developmental biology Copper Radioisotopes chemistry Positron emission tomography Positron-Emission Tomography 030220 oncology & carcinogenesis PARP inhibitor Cancer research Phthalazines Molecular Medicine Poly(ADP-ribose) Polymerases Molecular probe |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 27:3472-3476 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2017.05.077 |
| Popis: | Poly(ADP-ribose) polymerase (PARP) has emerged as an important molecular target for the treatment of several oncological diseases. A couple of molecular probes based on Olaparib scaffold have been developed by incorporation of F-18 or fluorophore for positron emission tomography (PET) or optical imaging in several types of tumor. PARP has been reported overexpressed in mesothelioma. We hereby synthesized an analogue of Olaparib containing DOTA moiety and radiolabeled it with Cu-64 to evaluate its utility of PET tracer for mesothelioma. The Cu-64 labeling was conveniently achieved at 90% yield with final compound at >99% radiochemistry purity. The biodistribution and PET imaging were performed at 0.5, 1, 2 and 18 h to confirm the in vivo tumor targeting. The tumor uptake in study group was significant higher than that in control group (3.45 ± 0.47% ID/g vs 2.26 ± 0.30% ID/g) and tumor were clearly detected by PET imaging. These results suggest the feasibility to develop an Olaparib-based theranostic agent for mesothelioma. |
| Databáze: | OpenAIRE |
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