Structure-activity studies of antagonists of luteinizing hormone-releasing hormone with emphasis on the amino-terminal region.
Structure-activity studies of antagonists of luteinizing hormone-releasing hormone with emphasis on the amino-terminal region.
复制标题
黄体生成素释放激素拮抗剂的结构活性研究，重点是氨基末端区域。
DOI：
10.1021/jm00387a029
复制
发表时间：
1987
影响因子：
7.3
通讯作者：
Coy,DH
中科院分区：
文献类型：
--
作者：
Hocart,SJ;Nekola,MV;Coy,DH
The structure-activity relationship of the hydrophobic amino terminal region of the antagonist [N-Ac-D-NaP. D-pClPhe2, D-Trp3, D-Arg6, Phe7, D-Ala10]-LH-RH has been investigated by the incorporation of a variety of amino acids with emphasis on positions 1, 2, and 3. The analogues were prepared by routine solid-phase peptide synthesis. All purifications were performed in two stages: gel permeation chromatography followed by preparative, reversed-phase, high-performance chromatography. The analogues were assayed in a standard rat anti ovulatory assay using a 40% propane-1, 2-diol-saline vehicle. A simplified antagonist was developed that allowed the removal of the customsynthesized D-pCIPhe and the labile D-Trp while retaining antiovulatory potency. The compound [N-Ac-d-Nal1, D-Phe2’3, D-Arg6, Phe7, D-Ala10]-LH-RH caused a 56% blockade of ovulation at the 500-ng dose and is approximately equipotent with the parent analogue inthis system.
