Synthesis and biological activity of peptide antagonists of luliberin (luteinizing hormone-releasing hormone).

作者信息

Moersch G W, Rebstock M C, Wittle E L, Tinney F J, Nicolaides E D, Hutt M P, Mich T F, Vandenbelt J M, Edgren R E, Reel J R, Dermody W C, Humphrey R R

出版信息

J Med Chem. 1979 Aug;22(8):935-43. doi: 10.1021/jm00194a010.

DOI:10.1021/jm00194a010

PMID:385877

Abstract

A series of des-His2 octa- and nonapeptide analogues of luliberin (luteinizing hormone-releasing hormone) with modifications in the 1 and 6 positions, and in some instances the 10 position, has been prepared. Some of these analogues are potent inhibitors of luliberin in vitro and in vivo. The use of ultraviolet absorption measurements for evaluating peptides containing tyrosine and tryptophan is described. An efficient synthesis of O-methyl-d-tyrosine is reported.

摘要