ACTH-Induced lipolysis in rat adipocytes: Structure-activity relationships
- 1 March 1978
- journal article
- research article
- Published by Springer Nature in Naunyn-Schmiedebergs Archiv für experimentelle Pathologie und Pharmakologie
- Vol. 302 (1) , 31-36
- https://doi.org/10.1007/bf00586593
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.Keywords
This publication has 21 references indexed in Scilit:
- Adrenal cortex adenylate cyclaseNaunyn-Schmiedebergs Archiv für experimentelle Pathologie und Pharmakologie, 1976
- Behaviourably active ACTH analoguesBiochemical Pharmacology, 1975
- Hormone-receptor interactions. Adrenocorticotropic hormone binding site increase in isolated fat cells by phenoxazonesBiochemistry, 1974
- Lipolytic activity of Met-Arg-His-Phe-Arg-Trp-Gly, a synthetic analog of the ACTH (4-10) core sequenceJournal of Medicinal Chemistry, 1973
- Adrenocorticotropin. Synthesis of [6-phenylalanine]-α1-19-adrenocorticotropic hormone and its steroidogenic, melanocyte-stimulating, and lipolytic activityBiochemistry, 1972
- Isolated adrenal cells: Steroidogenesis and cyclic AMP accumulation in response to ACTHArchives of Biochemistry and Biophysics, 1972
- Neurohypophyseal Hormone-Sensitive Adenyl Cyclase of Toad Urinary BladderProceedings of the National Academy of Sciences, 1970
- Threshold and Receptor Reserve in the Action of Neurohypophyseal PeptidesThe Journal of general physiology, 1970
- Abbreviated Designation of Amino Acid Derivatives and PeptidesEuropean Journal of Biochemistry, 1967
- Die Synthese eines Tetracosapeptides mit der Aminosäuresequenz eines hochaktiven Abbauproduktes des β‐Corticotropins (ACTH) aus Schweinehypophysen. (Vorläufige Mitteilung)Helvetica Chimica Acta, 1960