Poly(ADP-ribose) Polymerase in Neurodegeneration: Radiosynthesis and Radioligand Binding in ARC-SWE tg Mice.
Santosh R AlluriPatrick Johannes RissPublished in: ACS chemical neuroscience (2018)
We report the synthesis, radiosynthesis, and characterization of a radioligand for poly(ADP-ribose) polymerase (PARP). PARP is of central importance in cell homeostasis, neuroplasticity, and neurodegeneration in the brain. A radiolabeled PARP inhibitor was developed and used for autoradiographic quantification of PARP protein concentration in wild-type and transgenic rodent brains ex vivo in high resolution. The binding of [3H]rucaparib was found to be confined to PARP-expressing domains, for example, cerebellar cortex or hippocampal regions in both models. Saturation binding experiments confirmed selective and reversible binding to a single site ( Kd = 1.1 ± 0.2 nM).
Keyphrases
- dna damage
- dna repair
- wild type
- high resolution
- binding protein
- pet imaging
- dna binding
- single cell
- photodynamic therapy
- cell therapy
- white matter
- small molecule
- functional connectivity
- metabolic syndrome
- stem cells
- mesenchymal stem cells
- resting state
- adipose tissue
- computed tomography
- high fat diet induced
- insulin resistance
- structural basis
- brain injury
- high speed