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  • Title: New class of corticotropin-releasing factor (CRF) antagonists: small peptides having high binding affinity for CRF receptor.
    Author: Yamada Y, Mizutani K, Mizusawa Y, Hantani Y, Tanaka M, Tanaka Y, Tomimoto M, Sugawara M, Imai N, Yamada H, Okajima N, Haruta J.
    Journal: J Med Chem; 2004 Feb 26; 47(5):1075-8. PubMed ID: 14971886.
    Abstract:
    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-Ala31 and cyclohexylalanine38 on that surface was as potent as astressin in binding to the CRF receptor and showed significant ACTH suppression when administered to rats.
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