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. 2005 Mar;11(3):136-41.
doi: 10.1002/psc.599.

The design of a new potent and selective ligand for the orphan bombesin receptor subtype 3 (BRS3)

Robert G Boyle  1 , John Humphries, Tim Mitchell, Graham A Showell, Robert Apaya, Hiroaki Iijima, Hiroshi Shimada, Tomonori Arai, Hiroaki Ueno, Yoshihiro Usui, Toshiro Sakaki, Etsuko Wada, Keiji Wada
Affiliations

The design of a new potent and selective ligand for the orphan bombesin receptor subtype 3 (BRS3)

Robert G Boyle et al. J Pept Sci. 2005 Mar.

Abstract

Extensive SAR studies on the unselective BRS3 agonist, [H-D-Phe6,beta-Ala11,Phe13,Nle14]-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-Phe6,betaAla11,Phe13,Nle14]-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(tauBzl)-Nip-Gly-Arg-NH2.

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