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Conformationally constrained tachykinins: N‐methylated analogues of neurokinin A
Author(s) -
Rovero P.,
Pestellini V.,
Patacchini R.,
Santicioli P.,
Maggi C. A.,
Meli A.
Publication year - 1989
Publication title -
biopolymers
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.556
H-Index - 125
eISSN - 1097-0282
pISSN - 0006-3525
DOI - 10.1002/bip.360280109
Subject(s) - chemistry , peptide , selectivity , neurokinin b , neurokinin a , stereochemistry , receptor , methylation , sequence (biology) , substance p , biochemistry , neuropeptide , gene , catalysis
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.

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