Development of Peptide-Based Probes for Molecular Imaging of the Postsynaptic Density in the Brain

J Med Chem. 2024 Jul 25;67(14):11975-11988. doi: 10.1021/acs.jmedchem.4c00615. Epub 2024 Jul 9.

Abstract

The postsynaptic density (PSD) comprises numerous scaffolding proteins, receptors, and signaling molecules that coordinate synaptic transmission in the brain. Postsynaptic density protein 95 (PSD-95) is a master scaffold protein within the PSD and one of its most abundant proteins and therefore constitutes a very attractive biomarker of PSD function and its pathological changes. Here, we exploit a high-affinity inhibitor of PSD-95, AVLX-144, as a template for developing probes for molecular imaging of the PSD. AVLX-144-based probes were labeled with the radioisotopes fluorine-18 and tritium, as well as a fluorescent tag. Tracer binding showed saturable, displaceable, and uneven distribution in rat brain slices, proving effective in quantitative autoradiography and cell imaging studies. Notably, we observed diminished tracer binding in human post-mortem Parkinson's disease (PD) brain slices, suggesting postsynaptic impairment in PD. We thus offer a suite of translational probes for visualizing and understanding PSD-related pathologies.

MeSH terms

  • Animals
  • Autoradiography
  • Brain* / diagnostic imaging
  • Brain* / metabolism
  • Disks Large Homolog 4 Protein* / metabolism
  • Fluorine Radioisotopes / chemistry
  • Humans
  • Male
  • Molecular Imaging / methods
  • Molecular Probes / chemistry
  • Parkinson Disease / diagnostic imaging
  • Parkinson Disease / metabolism
  • Peptides / chemistry
  • Peptides / metabolism
  • Post-Synaptic Density* / metabolism
  • Pyridines
  • Pyrrolidinones
  • Rats
  • Rats, Sprague-Dawley
  • Tritium

Substances

  • Disks Large Homolog 4 Protein
  • Fluorine Radioisotopes
  • Peptides
  • Molecular Probes
  • Fluorine-18
  • 1-((3-(methylpyridin-4-yl)methyl)-4-(3,4,5-trifluorophenyl)pyrrolidin-2-one
  • Tritium
  • Pyridines
  • Pyrrolidinones