New Class of Corticotropin-Releasing Factor (CRF) Antagonists:Small Peptides Having High Binding Affinity for CRF Receptor

摘要

The discovery of small and potent peptide antagonists of the corticotropin-releasing factor (CRF) receptor is described.Through the structure-activity relationship studies of 12-amino acid peptide corresponding to the C-terminal residues of astressin,we assumed that a particular surface of the alpha-helix was important for binding to the receptor.The small peptide containing D-Ala~31 and cyclohexylalanine~38 on that surface was as potent as astressin in binding to the CRF receptor and showed significant ACTH suppression when administered to rats.