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 Enrico Schild and Pia Steen Petersen and Tom-Marten Kilian and Jacek Mokrosiński and Thomas M. Frimurer and Constance Chollet and Thue W. Schwartz and Birgitte Holst and Annette G Beck-Sickinger},
  journal={Journal of medicinal chemistry},
  year={2012},
  volume={55 17},
  pages={7437-49}
}
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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