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The design of a new potent and selective ligand for the orphan bombesin receptor subtype 3 (BRS3)
Author(s) -
Boyle Robert G.,
Humphries John,
Mitchell Tim,
Showell Graham A.,
Apaya Robert,
Iijima Hiroaki,
Shimada Hiroshi,
Arai Tomonori,
Ueno Hiroaki,
Usui Yoshihiro,
Sakaki Toshiro,
Wada Etsuko,
Wada Keiji
Publication year - 2005
Publication title -
journal of peptide science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.475
H-Index - 66
eISSN - 1099-1387
pISSN - 1075-2617
DOI - 10.1002/psc.599
Subject(s) - bombesin , agonist , chemistry , moiety , amide , stereochemistry , ligand (biochemistry) , receptor , orphan receptor , peptide , partial agonist , endogenous agonist , pharmacology , biochemistry , medicine , neuropeptide , transcription factor , dopamine receptor d1 , gene
Extensive SAR studies on the unselective BRS3 agonist, [H‐D‐Phe 6 ,β‐Ala 11 ,Phe 13 ,Nle 14 ]‐bombesin‐(6‐14)‐nonapeptide amide, have highlighted structural features important for BRS3 activity and have provided guidance as to the design of selective agonists. A radically modified heptapeptide agonist, maintaining only the Trp‐Ala moiety of the parent [H‐D‐Phe 6 ,βAla 11 ,Phe 13 ,Nle 14 ]‐peptide amide, and with a very different carboxyl terminal region, has been produced which was potent at BRS3 and essentially had no NMB or GRP receptor activity. Its structure is Ac‐Phe‐Trp‐Ala‐His(τBzl)‐Nip‐Gly‐Arg‐NH 2 . Copyright © 2004 European Peptide Society and John Wiley & Sons, Ltd.
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