Illuminating Neuropeptide Y Y₄ Receptor Binding: Fluorescent Cyclic Peptides with Subnanomolar Binding Affinity as Novel Molecular Tools.

ABSTRACT: The neuropeptide Y (NPY) Y₄ receptor (Y₄R), a member of the family of NPY receptors, is physiologically activated by the linear 36-amino acid peptide pancreatic polypeptide (PP). The Y₄R is involved in the regulation of various biological processes, most importantly pancreatic secretion, gastrointestinal motility, and regulation of food intake. So far, Y₄R binding affinities have been mostly studied in radiochemical binding assays. Except for a few fluorescently labeled PP derivatives, fluorescence-tagged Y₄R ligands with high affinity have not been reported. Here, we introduce differently fluorescence-labeled (Sulfo-Cy5, Cy3B, Py-1, Py-5) Y₄R ligands derived from recently reported cyclic hexapeptides showing picomolar Y

SUBMITTER: Gleixner J 

PROVIDER: S-EPMC11019746 | biostudies-literature | 2024 Apr

REPOSITORIES: biostudies-literature