Current studies center upon the metabolic breakdown of peptide hormones in various mammalian organs in vitro and in vivo, with particular focus on the renal handling of peptide hormones. The techniques employed include the radioactive labeling of peptide hormones, HPLC analysis of labeled products obtained after perfusion of labeled hormone through renal tubules, and vascular beds in comparison to the breakdown with isolated tissue enzymes. The information derived is applied in structure activity relationships with the view of designing highly active, enzymatically resistant LHRH antagonists capable of preventing ovulation and oxytocin antagonists capable of preventing preterm labor.

  
George Flouret
Professor
PhD University of Wisonsin
g-flouret@northwestern.edu
Morton 5-678
(312) 503-7965
 

Selected Publications:

Park SH, Song CH, Pak SC, Flouret G, Wilson L. (2000) The effect of oxytocin antagonist on uterus in response to exogenous oxytocin.J. Korean Med. Sci. 15:299-302.

Fejgin, M.D., Pak, S.C., Flouret, G., Parsons, M.T., Wilson, L. Jr. (1998) Comparison of the in vivo activity of different oxytocin antagonists in the pregnant baboon.J. Soc. Gynecol. Investig. 5: 251-254.

Flouret, G., Arnold, Z.S., Majewski, T., Petousis, N.H., Mahan, K., Farooqui, F., Blum, K.A., Konopinska, D., Natarajan, S. and Crich, D. (1995) Antiovulatory antagonists of LHRH related to antide. J. Pept. Sci. 1: 89-108.

Pak, S.C., Bertoncini, D., Meyer, W., Scaunas, D., Flouret, G. and Wilson, L. Jr (1994) Comparison of binding affinity of oxytocin antagonists to human and rat uterine oxytocin receptors and their correlation to the rat uterine oxytocic bioassay. Biol. Reprod. 51: 1140-1144.

Fejgin, M.D., Pak, S.C., Warnell, C., Flouret, G., Parsons, M.T., Wilson, L. Jr (1994) Oxytocin antagonist inhibitory effect on the rat and baboon uterus may be overcome by prostaglandins. Am. J. Obstet. Gynecol. 171: 1076-1080.

Flouret, G., Majewski, T., Brieher, W., Wilson, L. Jr (1993) Systematic substitution of an oxytocin antagonist with D-amino acids: unexpected high antagonistic potency of the D-Cys6-substituted analogue. J. Med. Chem. 36: 747-749.

Flouret, G., Mahan, K. and Majewski, T. (1992) Decreased histamine release by luteinizing hormone-releasing hormone antagonists obtained upon translocation of the cationic amino acid from position 8 to position 7. J. Med. Chem. 35: 636-640.

Flouret, G., Brieher, W., Mahan, K., Wilson, L. Jr (1991) Design of potent oxytocin antagonists featuring D-tryptophan at position 2. J. Med. Chem. 34: 642-646.

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