An aromatic region to induce a switch between agonism and inverse agonism at the ghrelin receptor.

@article{Els2012AnAR,
  title={An aromatic region to induce a switch between agonism and inverse agonism at the ghrelin receptor.},
  author={Sylvia Els and E. Schild and P. Petersen and Tom-Marten Kilian and J. Mokrosiński and T. Frimurer and Constance Chollet and T. Schwartz and B. Holst and A. Beck-Sickinger},
  journal={Journal of medicinal chemistry},
  year={2012},
  volume={55 17},
  pages={
          7437-49
        }
}
  • Sylvia Els, E. Schild, +7 authors A. Beck-Sickinger
  • Published 2012
  • Medicine, Chemistry
  • Journal of medicinal chemistry
  • The ghrelin receptor displays a high constitutive activity suggested to be involved in the regulation of appetite and food intake. Here, we have created peptides with small changes in the core binding motif -wFw- of the hexapeptide KwFwLL-NH(2) that can swap the peptide behavior from inverse agonism to agonism, indicating the importance of this sequence. Introduction of β-(3-benzothienyl)-d-alanine (d-Bth), 3,3-diphenyl-d-alanine (d-Dip) and 1-naphthyl-d-alanine (d-1-Nal) at position 2 resulted… CONTINUE READING
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