Peptide backbone modifications on the C-terminal hexapeptide of neurotensin

To compare backbone-induced susceptibilities with affinity changes that are caused by side-chain modifications in the respective positions, structure activity relationship studies on a series of NT(8-13) analogues were performed providing valuable insights into the major requirement for neurotensin receptor recognition and activation. The data led us to highly potent NTR1 ligands and the generation of a pharmacophore model that will be helpful for the discovery of therapeutically relevant non-peptidic NTR1 agonists.

Graphical abstractHighly potent neurotensin receptor ligands and the generation of a pharmacophore model are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide