Abstract:
:The role of the D-Trp residues in the sequence of the NK2-selective tachykinin antagonist, MEN 10207 (Asp-Tyr-D-Trp-Val-D-Trp-D-Trp-Arg-NH2). has been examined by replacement of each D-Trp with either the L-isomer or the residue naturally occurring in the same position of neurokinin A(4-10). The biological activity of the analogues thus obtained has been characterized, with special attention to the selectivity for the three tachykinin receptors and for the two subtypes of the NK2 receptor recently described. We conclude that the simultaneous presence of the three D-Trp residues of MEN 10207 is crucial both for affinity and for selectivity.
journal_name
Peptidesjournal_title
Peptidesauthors
Rovero P,Astolfi M,Renzetti AR,Patacchini R,Giachetti A,Maggi CAdoi
10.1016/0196-9781(91)90053-rsubject
Has Abstractpub_date
1991-09-01 00:00:00pages
1015-8issue
5eissn
0196-9781issn
1873-5169pii
0196-9781(91)90053-Rjournal_volume
12pub_type
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