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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 

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

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.[1]

References

  1. The design of a new potent and selective ligand for the orphan bombesin receptor subtype 3 (BRS3). Boyle, R.G., Humphries, J., Mitchell, T., Showell, G.A., Apaya, R., Iijima, H., Shimada, H., Arai, T., Ueno, H., Usui, Y., Sakaki, T., Wada, E., Wada, K. J. Pept. Sci. (2005) [Pubmed]
 
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