Further structure-activity studies of lactam derivatives of MT-II and SHU-9119: their activity and selectivity at human melanocortin receptors 3, 4, and 5.

@article{Grieco2007FurtherSS,
  title={Further structure-activity studies of lactam derivatives of MT-II and SHU-9119: their activity and selectivity at human melanocortin receptors 3, 4, and 5.},
  author={Paolo Grieco and Minying Cai and Guoxia Han and Dev B Trivedi and Pietro Campiglia and Ettore Novellino and Victor J. Hruby},
  journal={Peptides},
  year={2007},
  volume={28 6},
  pages={1191-6}
}
Recently we have demonstrated that replacing His(6) by constrained amino acids(2) in the well-known antagonist SHU-9119 resulted in potent and selective antagonist ligands especially at the hMC3R and hMC5 receptors. With the aim to further explore position 6 in the sequence of SHU-9119 and MT-II, we have designed, synthesized, and pharmacologically characterized a series of peptide analogues of MT-II and SHU-9119 at the human melanocortin receptors subtypes MC3R, MC4R and MC5R. All these… CONTINUE READING