Syntheses by the conventional methods as well as the chemical, physical and biological properties are described of the following analogs of the LH-releasing hormone (LH-RH): [Leu3]-LH-RH, [Phe3]-LH-RH, [Trp2] [His3]-LH-RH, Des-Trp3-LH-RH, Des-His2-[Phe5]-LH-RH, [Ala4]-LH-RH, [Phe5]-LH-RH and [Ala4] [Phe5]-LH-RH. In vivo assays showed that [Leu3]-LH-RH did not release LH in doses as high as 5 - 25 μg, having less than 0.0008% of LH-RH activity, while [Phe3]-LH-RH had 0.43% of the LH-RH activity of natural LH-RH. The LH-RH activities of [Trp2] [His3]-LH-RH, Des-Trp3-LH-RH and Des-His2-[Phe5]-LH-RH were extremely low. On the other hand, [Ala4]-LH-RH, [Phe5]-LH-RH and [Ala4] [Phe5]-LH-RH had significant LH-RH activity. The structure-activity relationship of LH-RH is discussed on the basis of these findings.
|Original language||English (US)|
|Number of pages||10|
|Journal||Biochemical and biophysical research communications|
|State||Published - May 1 1973|
ASJC Scopus subject areas
- Molecular Biology
- Cell Biology