Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R.

@article{HaskellLuevano1997DiscoveryOP,
  title={Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R.},
  author={Carrie Haskell-Luevano and Siska Hendrata and Cheryl North and Tomi K. Sawyer and Mac E. Hadley and Victor J. Hruby and C Dickinson and Ira Gantz},
  journal={Journal of medicinal chemistry},
  year={1997},
  volume={40 14},
  pages={
          2133-9
        }
}
[Nle4, DPhe7]-alpha-MSH (NDP-MSH), a highly potent analogue of alpha-melanocyte-stimulating hormone (alpha-MSH), possesses nanomolar efficacies at all the melanocortin receptor subtypes except the MC2R. Evaluation of the melanocortin "message" sequence of [Nle4, DPhe7]-alpha-MSH was performed on the human melanocortin receptor subtypes designated hMC1, hMC3R, hMC4R, and hMC5R. Tetrapeptides and tripeptides were stereochemically modified to explore topochemical preferences at these receptors and… CONTINUE READING

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