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High-Affinity and Proteolytically Stable Peptidic Fluorescent NTS1R Ligands.

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New fluorescent ligands targeting neurotensin receptor 1 (NTS1R) show high binding affinity and stability. These probes are valuable tools for studying NTS1R expression and binding in cells and tumors.

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Area of Science:

  • Medicinal Chemistry
  • Neuroscience
  • Molecular Imaging

Background:

  • Neurotensin receptor 1 (NTS1R) is implicated in CNS disorders, gastrointestinal functions, and cancer.
  • Development of high-affinity, stable, and fluorescent ligands is crucial for NTS1R research.
  • Existing ligands often lack sufficient stability or binding characteristics for detailed investigation.

Purpose of the Study:

  • To synthesize novel fluorescence-labeled neurotensin(8-13) analogs as high-affinity NTS1R ligands.
  • To enhance proteolytic stability and binding affinity of neurotensin-derived probes.
  • To validate the utility of these probes for NTS1R expression analysis and imaging.

Main Methods:

  • Chemical modification of neurotensin(8-13) sequence, including amino-functionalized carbamoylated arginine at position 8, Nα-methylation, and specific amino acid substitutions (Tyr11, Leu13).
  • Conjugation of fluorophores (5-TAMRA, sulfo-Cy5) to the modified peptide backbone.
  • Assessment of binding affinity (Ki), plasma stability (t1/2), and application in flow cytometry and confocal microscopy for cellular and tissue imaging.

Main Results:

  • Synthesized fluorescent NTS1R ligands (e.g., 5-TAMRA-ligand 19, sulfo-Cy5 probe 21) exhibit unprecedented binding affinity (Ki as low as 0.094 nM).
  • Probes demonstrate high stability in human plasma (t1/2 >> 48 h).
  • Successful application in competition binding studies, imaging NTS1R in living cells, and visualizing NTS1R in tumor tissue.

Conclusions:

  • The developed fluorescent ligands represent a significant advancement for NTS1R research.
  • These probes offer superior affinity and stability, enabling more accurate investigation of NTS1R.
  • The study validates their potential for diagnostic and research applications in oncology and neuroscience.