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Structure−Activity Relationships of a Series of Analogs of the Endozepine Octadecaneuropeptide (ODN 11 - 18 ) on Neurosteroid Biosynthesis by Hypothalamic Explants

Abstract : We have previously shown that the endozepine octadecaneuropeptide (ODN) stimulates the biosynthesis of neurosteroids from frog hypothalamic explants. In the present study, we have investigated the structure-activity relationships of a series of analogs of the C-terminal octapeptide of ODN (OP) on neurosteroid formation. We found that OP and its cyclic analog cyclo1-8OP stimulate in a concentration-dependent manner the synthesis of various steroids including 17-hydroxypregnenolone, progesterone, 17-hydroxyprogesterone and dehydroepiandrosterone. Deletion or Ala-substitution of the Arg1 or Pro2 residues of OP did not affect the activity of the peptide. In contrast, deletion or replacement of any of the amino acids of the C-terminal hexapeptide fragment totally abolished the effect of OP on neurosteroid biosynthesis. The present study indicates that the C-terminal hexapeptide of ODN/OP is the minimal sequence retaining full biological activity on steroid-producing neurons.
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https://hal-normandie-univ.archives-ouvertes.fr/hal-01962719
Contributor : Jérôme Leprince <>
Submitted on : Thursday, December 20, 2018 - 6:02:14 PM
Last modification on : Monday, July 20, 2020 - 1:06:06 PM

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Jean Luc Do Rego, Jérôme Leprince, Van Luu-The, Georges Pelletier, Marie-Christine Tonon, et al.. Structure−Activity Relationships of a Series of Analogs of the Endozepine Octadecaneuropeptide (ODN 11 - 18 ) on Neurosteroid Biosynthesis by Hypothalamic Explants. Journal of Medicinal Chemistry, American Chemical Society, 2007, 50 (13), pp.3070-3076. ⟨10.1021/jm0610548⟩. ⟨hal-01962719⟩

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