The objectives of this contract are to design, synthesize and test peptide antagonists which have very low histamine releasing properties (equivalent to LHRH, or less) and which completely inhibit ovulation in rats, s.c., at one-tenth the dose of the most potent antagonists currently available, such as Nal-Glu or Antide. Such antagonists should, desirably, also be devoid of (or have minimal) ancillary endocrine, central nervous system, cardiovascular and other side effects.
| Janecka, A; Janecki, T; Bowers, C Y et al. (1994) New, highly active antagonists of LHRH with acylated lysine and p-aminophenylalanine in positions 5 and 6. Int J Pept Protein Res 44:19-23 |
| Janecka, A; Janecki, T; Shan, S M et al. (1994) Novel, potent luteinizing hormone-releasing hormone antagonists with improved solubility in water. J Med Chem 37:2238-41 |
| Ljungqvist, A; Bowers, C Y; Folkers, K (1993) Synthesis and bioassay of LHRH-antagonists with N-Ac-D-O-phenyltyrosine and N-Ac-D-3-(2-dibenzofuranyl)alanine in position 1. Int J Pept Protein Res 41:427-32 |
| Janecka, A; Ljungqvist, A; Bowers, C et al. (1991) Superiority of an antagonist of the luteinizing hormone releasing hormone with emphasis on arginine in position 8, named Argtide. Biochem Biophys Res Commun 180:374-9 |
