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  • Title: ACTH-induced lipolysis in rat adipocytes: structure-activity relationships.
    Author: Opmeer FA, van Ree JM, de Wied D.
    Journal: Naunyn Schmiedebergs Arch Pharmacol; 1978 Mar; 302(1):31-6. PubMed ID: 206844.
    Abstract:
    The lipolytic action of natural porcine ACTH1(-39) and of a number of highly purified synthetic ACTH peptide fragments was studied using rat adipocytes. Of the analogues tested, only ACTH1(-24) exhibited full lipolytic activity with respect to intrinsic activity and affinity. Several shorter fragments appeared to be full agonists but had lower affinity. Fragments ACTH5(-10) and ACTH7(-10) were inactive. No antagonistic effects against the lipolytic action of ACTH could be demonstrated with substimulatory doses of ACTH1(-16), ACTH1(-10), ACTH7(-24) and ACTH11(-24). Based on the relative potency derived from dose-response curves, a more refined model with respect to the active centers being encoded in various sequences of the hormone, is proposed.
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