Selectivity of cyclic [D-Nal7] and [D-Phe7] substituted MSH analogues for the melanocortin receptor subtypes.

@article{Schith1997SelectivityOC,
  title={Selectivity of cyclic [D-Nal7] and [D-Phe7] substituted MSH analogues for the melanocortin receptor subtypes.},
  author={Helgi B. Schi{\"o}th and R M{\"u}ceniece and Felikss Mutulis and Peteris Prusis and Gunnar G Lindeberg and Som Datt Sharma and Victor J. Hruby and Jarl E. S. Wikberg},
  journal={Peptides},
  year={1997},
  volume={18 7},
  pages={1009-13}
}
The binding of the 2 cyclic lactam MSH (4-10) analogues (MTII, SHU9119), and 5 cyclic [Cys4, Cys10] alpha-MSH analogues were tested on cells transiently expressing the human MC1, MC3, MC4 and MC5 receptors. The results indicate a differential importance of the C-terminal (Lys-Pro-Val) and N-terminal (Ser-Tyr-Ser) of cyclic [Cys4, Cys10] alpha-MSH analogues in binding to the MC receptor subtypes. Substitution of D-Phe7 by D-Nal(2')7 in both the cyclic lactam MSH (4-10) and the cyclic disulphide… CONTINUE READING

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