Structure-activity studies on the corticotropin releasing factor antagonist astressin, leading to a minimal sequence necessary for antagonistic activity.

@article{Rijkers2004StructureactivitySO,
  title={Structure-activity studies on the corticotropin releasing factor antagonist astressin, leading to a minimal sequence necessary for antagonistic activity.},
  author={Dirk T. S. Rijkers and John A. W. Kruijtzer and Marja van Oostenbrugge and Eric Ronken and Jack A J den Hartog and Rob M. J. Liskamp},
  journal={Chembiochem : a European journal of chemical biology},
  year={2004},
  volume={5 3},
  pages={340-8}
}
Corticotropin Releasing Factor (CRF) antagonists are considered promising for treatment of stress-related illnesses such as major depression and anxiety-related disorders. We report here the design, synthesis and biological evaluation of 91 truncated astressin analogues in order to deduce the pharmacophoric amino acid residues. Such truncated peptides may serve as valuable lead structures for the development of new small, non-peptide-based CRF antagonists. N-Terminal truncation of astressin led… CONTINUE READING