title: Conformationally constrained tachykinins: N-methylated analogues of neurokinin A.
abstract: Limited conformational constraints have been introduced in the sequence of the C-terminal fragment of the peptide neurotransmitter neurokinin A by N-methylation of individual peptide bonds, and the biological activities of the peptides thus obtained were evaluated in order to assess the effect of such conformational constraint on receptor selectivity. The analogue methylated in position 7 shows enhanced selectivity toward NK-1 receptor.
authors.forename: P
authors.initials: P
authors.lastname: Rovero
authors.forename: V
authors.initials: V
authors.lastname: Pestellini
authors.forename: R
authors.initials: R
authors.lastname: Patacchini
authors.forename: P
authors.initials: P
authors.lastname: Santicioli
authors.forename: C A
authors.initials: CA
authors.lastname: Maggi
authors.forename: A
authors.initials: A
authors.lastname: Meli
mesh_terms: D000595:Amino Acid Sequence; D008745:Methylation; D008969:Molecular Sequence Data; D015288:Neurokinin A / Q000031:analogs & derivatives*; D009842:Oligopeptides / Q000138:chemical synthesis; D011487:Protein Conformation
chemical_list: D009842:Oligopeptides; D015288:Neurokinin A