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Guiding principles applied in the design of GPCR-selective hypothalamic hormone agonists and antagonists

  • Conference paper
Insights into Receptor Function and New Drug Development Targets

Part of the book series: Research and Perspectives in Endocrine Interactions ((RPEI))

  • 518 Accesses

Summary

Strategies for the design of peptide agonists and antagonists of gonadotropin releasing hormone (GnRH, one ligand and one receptor) and of receptor-selective agonists and antagonists of somatostatin (SRIF, three ligands and five receptors) and corticotropin releasing factor (CRF, three ligands and two receptors) are described. These strategies include the use of unusual amino acids, a versatile scaffold based on aminoglycine (betidamino acids) and side chain as well as backbone conformational constraints.

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Authors and Affiliations

  1. The Clayton Foundation Laboratories for Peptide Biology, The Salk Institute, La Jolla, CA

    J. Rivier, J. Gulyas, J. Erchegyi, S. C. Koerber, M. DiGruccio, M. Perrin, C. Rivier & W. Vale

  2. Structural Biology Laboratory, The Salk Institute, La Jolla, CA

    C. R. R. Grace & R. Riek

  3. Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Berne, Switzerland

    V. Eltschinger, B. Waser, R. Cescato & J. C. Reubi

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  1. J. Rivier
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Editors and Affiliations

  1. Divisions of Neuroscience and Reproductive Biology, Departments of Physiology and Pharmacology and Cell and Developmental Biology, Oregon National Primate Research Center, Oregon Health and Science University, 505 NW 185th Avenue, Beaverton, Oregon, 97006, USA

    Michael Conn Ph.D.

  2. Institut Necker, 156, rue de Vaugirard, 75015, Paris, France

    Claude Kordon Ph.D.

  3. Pour la Recherche Thérapeutique, Fondation IPSEN, 24, rue Erlanger, 75781, Paris Cedex 16, France

    Yves Christen Ph.D.

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© 2006 Springer-Verlag Berlin Heidelberg

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Rivier, J. et al. (2006). Guiding principles applied in the design of GPCR-selective hypothalamic hormone agonists and antagonists. In: Conn, M., Kordon, C., Christen, Y. (eds) Insights into Receptor Function and New Drug Development Targets. Research and Perspectives in Endocrine Interactions. Springer, Berlin, Heidelberg . https://doi.org/10.1007/3-540-34447-0_8

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