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Synthesis and biological activities of analogs of luteinizing hormone-releasing hormone (LH-RH) substituted in position 1 or 2
Authors:N Yanihara  K Tsuji  C Yanaihara  T Hashimoto  T Kaneko  A Arimura  A V Schally
Affiliation:1. VA Hospital New Orleans, La., USA;2. Tulane University, School of Medicine, New Orleans, La., USA
Abstract:Syntheses are described of [Pro1]-LH-RH, [Orotic acid1]-LH-RH, [Glu1]-LH-RH, [Ser2]-LH-RH, [Leu2]-LH-RH, [Gln2]-LH-RH and [Phe2]-LH-RH. The LH-releasing hormone (LH-RH) activity of each of these peptides was compared with that of natural LH-RH in vivo. [Glu1]-LH-RH and [Phe2]-LH-RH had significant LH-RH activity, while all the other analogs possessed extremely low activities. These findings are briefly discussed in the light of the structure-activity relationship for LH-RH.
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