The role of N-acyl groups in the inhibitory activity of LH-RH analogues

Imre Mezö, János Seprödi, Judit Érchegyi, István Teplán, Magdolna Kovacs, Bela Flerkó

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2 Citations (Scopus)

Abstract

Inhibitory analogues of luteinizing hormone-releasing hormone (LH-RH) were prepared with formyl-D-Trp1, acetyl-D-Trp1, valeryl-D-Trp1, tartaryl-D-Trp1, diacetyl-tartaryl-D-Trp1, acetyl-Gly1, and acetyl-Sar1 successively replacing the position one in the analogue [D-Trp1, D-p-Cl-Phe2, D-Trp3, D-Phe6, D-Ala10]-LH-RH. The formyl-D-Trp1 and acetyl-D-Trp1 analogues yielded 100% blockade of ovulation at the 10 μg dose; the others were less potent and inhibited ovulation at the 50 μg dose. The inhibitory potency seems to correlate with the polarity of the acyl group.

Original languageEnglish
Pages (from-to)149-151
Number of pages3
JournalPeptides
Volume4
Issue number2
DOIs
Publication statusPublished - Jan 1 1983

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Keywords

  • Inhibition of ovulation
  • LH-RH
  • LH-RH inhibitors
  • Solid phase peptide synthesis

ASJC Scopus subject areas

  • Biochemistry
  • Physiology
  • Endocrinology
  • Cellular and Molecular Neuroscience

Cite this

Mezö, I., Seprödi, J., Érchegyi, J., Teplán, I., Kovacs, M., & Flerkó, B. (1983). The role of N-acyl groups in the inhibitory activity of LH-RH analogues. Peptides, 4(2), 149-151. https://doi.org/10.1016/0196-9781(83)90105-5