Can I read Systematic optimization of a lead-structure identities for a selective short peptide agonist for the human orphan receptor BRS-3 on EtoBox?

Systematic optimization of a lead-structure identities for a selective short peptide agonist for the human orphan receptor BRS-3 by Dirk Weber; Claudia Berger; Timo Heinrich; Peter Eickelmann; Jochen Antel; Horst Kessler is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is Systematic optimization of a lead-structure identities for a selective short peptide agonist for the human orphan receptor BRS-3 about?

The orphan receptor, human bombesin receptor subtype 3 (BRS-3) was assigned to the G-protein coupled bombesin receptor family because of its high sequence homology with the neuromedin B receptor (NMB-R) and gastrin-releasing peptide receptor (GRP-R). Since its pharmacology is stiIl unknown, new highly potent and selective tool-substances are needed, that may be able to elucidate its possible role in obesity and cancer. We have performed structure activity relationship studies on the high affinity peptide agonists [D-Phe6,beta-Ala11,Phe13,Nle14]Bn(6-14) and [D-Phe6,Phe13]Bn(6-13)propylamide, using their ability to mobilize intracellular calcium in BRS-3 transfected CHOGa-16 cells combined with receptor binding studies. It was demonstrated that for [D-Phe,beta-Ala11,Phe13,Nle14]Bn(6-14) the side chains of the residues Trp8 and Phe13, and to a smaller extent beta-Ala11, are the important amino acid side chains for receptor activation and binding, however for [D-Phe6,Phe13]Bn(6-13) propylamide His12 seems to be more important than Phe13. C-and N-terminal deletions and amino acid substitutions allowed further understanding. It was demonstrated that substitution of His 12 by Tyr leads to

Who reads Systematic optimization of a lead-structure identities for a selective short peptide agonist for the human orphan receptor BRS-3?

Author

Dirk Weber; Claudia Berger; Timo Heinrich; Peter Eickelmann; Jochen Antel; Horst Kessler

Publisher

John Wiley and Sons; Wiley (John Wiley & Sons); John Wiley & Sons Inc.; Wiley (ISSN 1075-2617)

Published

2002

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)