论文部分内容阅读
用固相法合成了ｈＦ－ＧＲＰ及其１５个类似物。全部裂解均用三氟甲磺酸完成。产物总收率６０％～８０％。对所有合成肽进行了影响离体的小鼠垂体分泌ＬＨ的活性筛选。结果表明，当合成肽的浓度为０．０５ｍｍｏｌ／Ｌ时：（１）将ｈＦ－ＧＲＰ的Ｃ端ＣＯＯＨ变成ＣＯＮＨ２，活性变化不大；（２）Ｃ端残基Ａｓｎ１４被Ｐｈｅ替换后刺激垂体分泌ＬＨ的活性明显高于ｈＦ－ＧＲＰ；（３）Ｔｈｒ３被Ｔｙｒ替换后片段ｈＦ－ＧＲＰ（３～１３）有抑制ＬＨ分泌的活性；（４）其余类似物与空白对照相似。
HF-GRP and its 15 analogues were synthesized by solid phase method. All cleavage is accomplished with triflic acid. The total yield of 60% to 80%. All synthesized peptides were subjected to an activity screening of LH secretion secreted by pituitary in mice. The results showed that when the concentration of synthetic peptide was 0.05 mmol / L, (1) the activity of C-terminal COOH of hF-GRP was changed to CONH2 with little change in activity; (2) Asn14 (3) The hF-GRP fragment (3 ~ 13) after the replacement of Thr3 by Tyr could inhibit the secretion of LH; (4) The rest of the analogues were similar to the blank control.