LH-RH antagonists: Further analogs with ring-substituted aromatic residues

Judit Erchegi, David H. Coy, Mary V. Nekola, Escipion Pedroza, Esther J. Coy, Imre Mezo, Andrew V. Schally

Research output: Contribution to journalArticle

13 Scopus citations

Abstract

Although the systematic substitution of benzene and other aromatic ring systems with various atoms and groups has been a standard approach in conventional pharmaceutical research, it has only recently received the attention it deserves in peptide research. The observation that D-p-Cl-Phe inserted in position 2 of certain LH-RH (luteinizing hormone-releasing hormone) analogs results in large improvements in antagonist activity led us to examine the effect of this and other substituents on position 1 and 2 D-phenylalanyl analog side chains. Analogs containing two D-p-Cl-phenylalanines were found to be particularly powerful competitive inhibitors when assayed in cycling rat for blockade of ovulation. Analogs with non-aromatic amino acids in the first position exhibited much lower activities.

Original languageEnglish (US)
Pages (from-to)251-253
Number of pages3
JournalPeptides
Volume2
Issue number3
DOIs
StatePublished - Jan 1 1981
Externally publishedYes

Keywords

  • Anti-ovulatory studies
  • LH-RH antagonists
  • Ring-substituted-phenylalanines

ASJC Scopus subject areas

  • Biochemistry
  • Endocrinology
  • Physiology
  • Cellular and Molecular Neuroscience

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  • Cite this

    Erchegi, J., Coy, D. H., Nekola, M. V., Pedroza, E., Coy, E. J., Mezo, I., & Schally, A. V. (1981). LH-RH antagonists: Further analogs with ring-substituted aromatic residues. Peptides, 2(3), 251-253. https://doi.org/10.1016/S0196-9781(81)80114-3