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 language | English (US) |
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Pages (from-to) | 251-253 |
Number of pages | 3 |
Journal | Peptides |
Volume | 2 |
Issue number | 3 |
DOIs | |
State | Published - Jan 1 1981 |
Externally published | Yes |
Keywords
- Anti-ovulatory studies
- LH-RH antagonists
- Ring-substituted-phenylalanines
ASJC Scopus subject areas
- Biochemistry
- Endocrinology
- Physiology
- Cellular and Molecular Neuroscience