title: Peptide backbone modifications on the C-terminal hexapeptide of neurotensin.
abstract: 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.
authors.affiliation: Department of Chemistry and Pharmacy, Emil Fischer Center, Friedrich Alexander University, D-91052 Erlangen, Germany.
authors.forename: Jürgen
authors.initials: J
authors.lastname: Einsiedel
authors.forename: Harald
authors.initials: H
authors.lastname: Hübner
authors.forename: Maud
authors.initials: M
authors.lastname: Hervet
authors.forename: Steffen
authors.initials: S
authors.lastname: Härterich
authors.forename: Susanne
authors.initials: S
authors.lastname: Koschatzky
authors.forename: Peter
authors.initials: P
authors.lastname: Gmeiner
mesh_terms: D000818:Animals; D002118:Calcium / Q000378:metabolism; D015394:Molecular Structure; D016297:Mutagenesis, Site-Directed; D009154:Mutation / Q000235:genetics; D009496:Neurotensin / Q000737:chemistry* / Q000378:metabolism; D010165:Palladium / Q000494:pharmacology; D010446:Peptide Fragments / Q000737:chemistry*; D011485:Protein Binding; D012333:RNA, Messenger / Q000235:genetics / Q000378:metabolism; D018028:Receptors, Neurotensin / Q000235:genetics / Q000378:metabolism*; D020133:Reverse Transcriptase Polymerase Chain Reaction; D013329:Structure-Activity Relationship; D013552:Swine
chemical_list: D010446:Peptide Fragments; D012333:RNA, Messenger; D018028:Receptors, Neurotensin; C114036:neurotensin type 1 receptor; D009496:Neurotensin; D010165:Palladium; D002118:Calcium