title: The design of a new potent and selective ligand for the orphan bombesin receptor subtype 3 (BRS3).
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.
authors.affiliation: Astex Technology Ltd, Cambridge, UK. b.boyle@astex-technology.com
authors.forename: Robert G
authors.initials: RG
authors.lastname: Boyle
authors.forename: John
authors.initials: J
authors.lastname: Humphries
authors.forename: Tim
authors.initials: T
authors.lastname: Mitchell
authors.forename: Graham A
authors.initials: GA
authors.lastname: Showell
authors.forename: Robert
authors.initials: R
authors.lastname: Apaya
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Iijima
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Shimada
authors.forename: Tomonori
authors.initials: T
authors.lastname: Arai
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Ueno
authors.forename: Yoshihiro
authors.initials: Y
authors.lastname: Usui
authors.forename: Toshiro
authors.initials: T
authors.lastname: Sakaki
authors.forename: Etsuko
authors.initials: E
authors.lastname: Wada
authors.forename: Keiji
authors.initials: K
authors.lastname: Wada
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D001839:Bombesin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry; D002460:Cell Line; D015195:Drug Design; D006801:Humans; D008024:Ligands; D051379:Mice; D008958:Models, Molecular; D008969:Molecular Sequence Data; D011487:Protein Conformation; D018004:Receptors, Bombesin / Q000819:agonists* / Q000378:metabolism*; D013379:Substrate Specificity
chemical_list: D008024:Ligands; D018004:Receptors, Bombesin; C107120:bombesin receptor subtype 3; D001839:Bombesin