Abstract

The objectives of this contract are to design, synthesize and test LHRH antagonists with low (or no) histamine releasing properties and high antagonist potency utilizing data obtained from NMR and binding affinity studies as well as computer simulation techniques.

  Funding Agency

Agency
National Institute of Health (NIH)
Institute
Eunice Kennedy Shriver National Institute of Child Health & Human Development (NICHD)
Type
Research and Development Contracts (N01)
Project #
N01HD092903-001
Application #
2316451
Study Section
Project Start
1989-01-01
Project End
1990-10-31
Budget Start
1989-09-29
Budget End
1990-10-31
Support Year
Fiscal Year
1989
Total Cost
Indirect Cost

  Institution

Name
Salk Institute for Biological Studies
Department
Type
DUNS #
005436803
City
La Jolla
State
CA
Country
United States
Zip Code
92037

  Publications

Rivier, J; Jiang, G C; Lahrichi, S L et al. (1996) Dose relationship between GnRH antagonists and pituitary suppression. Hum Reprod 11 Suppl 3:133-47
Rivier, J E; Jiang, G; Porter, J et al. (1995) Gonadotropin-releasing hormone antagonists: novel members of the azaline B family. J Med Chem 38:2649-62
Rivier, J; Porter, J; Hoeger, C et al. (1992) Gonadotropin-releasing hormone antagonists with N omega-triazolylornithine, -lysine, or -p-aminophenylalanine residues at positions 5 and 6. J Med Chem 35:4270-8
Koerber, S C; Ibea, M; Hagler, A T et al. (1992) Synthesis and theoretical conformational studies of gonadotropin-releasing hormone analogs containing tetrahydroisoquinoline carboxylic acid. Biochem Biophys Res Commun 187:1035-41
Theobald, P; Porter, J; Rivier, C et al. (1991) Novel gonadotropin-releasing hormone antagonists: peptides incorporating modified N omega-cyanoguanidino moieties. J Med Chem 34:2395-402
Rivier, J; Theobald, P; Porter, J et al. (1991) Gonadotropin releasing hormone antagonists: novel structures incorporating N omega-cyano modified guanidine moieties. Biochem Biophys Res Commun 176:406-12