Literature DB >> 6385974

Antagonists of the luteinizing hormone releasing hormone (LHRH) with emphasis on the TRP7 of the salmon and chicken II LHRH's.

K Folkers, C Y Bowers, H M Shieh, Y Z Liu, S B Xiao, P F Tang, J Y Chu.   

Abstract

The sequences of four naturally occurring luteinizing hormone releasing hormones (LHRH's) differ only in positions 5, 7 and 8. Salmon and chicken II LHRH's have Trp7; porcine/ovine (P/O) and chicken I LHRH's have Leu7. The receptor for P/O LHRH might effectively bind certain antagonists with Trp7. Thirteen antagonists having Trp7 and eight antagonists with other substitutions in position 7 were synthesized. One of the thirteen antagonists with the natural Trp7, [N-Ac-D-2-Nal1,D-pClPhe2,D-3-Pal3,D-Arg6,Trp7,D- Ala10]-LHRH, not only maintained activity, but had increased potency (ca. 58%; 90% antiovulatory activity/250 ng; rats) in comparison with the companion analog with the natural Leu7 of P/O LHRH. The other twelve Trp7-antagonists had lower potency.

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Year:  1984        PMID: 6385974     DOI: 10.1016/s0006-291x(84)80263-6

Source DB:  PubMed          Journal:  Biochem Biophys Res Commun        ISSN: 0006-291X            Impact factor:   3.575


  2 in total

1.  Antide and related antagonists of luteinizing hormone release with long action and oral activity.

Authors:  A Ljungqvist; D M Feng; W Hook; Z X Shen; C Bowers; K Folkers
Journal:  Proc Natl Acad Sci U S A       Date:  1988-11       Impact factor: 11.205

2.  Decapeptides as effective agonists from L-amino acids biologically equivalent to the luteinizing hormone-releasing hormone.

Authors:  K Folkers; C Y Bowers; P F Tang; M Kubota
Journal:  Proc Natl Acad Sci U S A       Date:  1986-02       Impact factor: 11.205

  2 in total

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