Schafer D J, Black A D, Bower J D
J Med Chem. 1975 Jun;18(6):613-9. doi: 10.1021/jm00240a018.
Syntheses of the decapeptide luteinizing hormone-releasing hormone, less thanGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2 are described. The basic properties of arginine can provide a simple repetitive isolation procedure for arginine-containing peptides. The biological activities of the decapeptide, of a range of fragments and modified fragments, and of two analogs with alteration in the series at position 4 were measured by in vitro incubation with sheep pituitary slices, measuring the liberated LH by bioassay. None of the compounds of shortened sequence were active, with the exception of less thanGlu-His-Trp which showed 1% of the decapeptide in one of four experiments. Neither [Ser(But)4]-LH-RH-nor [Leu4]-LH-RH showed significant activity indicating (despite the known activity of [Ala4]-LH-RH) the importance of this part of the structure for full biological activity.
本文描述了少于Glu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2的十肽促黄体生成激素释放激素的合成。精氨酸的基本特性可为含精氨酸的肽提供一种简单的重复分离方法。通过与羊垂体切片进行体外孵育，并通过生物测定法测量释放的促黄体生成素（LH），测定了十肽、一系列片段和修饰片段以及两个在第4位序列发生改变的类似物的生物活性。除了少于Glu-His-Trp在四个实验之一中显示出十肽1%的活性外，缩短序列的化合物均无活性。[Ser(But)4]-LH-RH和[Leu4]-LH-RH均未显示出显著活性，这表明（尽管已知[Ala4]-LH-RH具有活性）该结构部分对于完整生物活性的重要性。
