Structure and function relationships of three novel hGHRH-GGC analogs

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• 作者：Song-Shan Tang ; Ming-Hua Du ; Juan-Hui Zhang ; Xin Kong ; Jing-Jing Liu
• 关键词：Growth hormone releasing hormone analogs ; Structure and function relationship ; Pro-Pro-hGHRH(1– ; 44)-Gly-Gly-Cys ; Pro-hGHRH(1– ; 44)-Gly-Gly-Cys ; ¹Pro-hGHRH(2– ; 44)-Gly-Gly-Cys ; Pituitary
• 刊名：Regulatory Peptides
• 出版年：2010
• 出版时间：8 January 2010
• 年：2010
• 卷：159
• 期：1-3
• 页码：87-92
• 全文大小：359 K

文摘

Growth hormone releasing hormone (GHRH) is one of the hypothalamus hormones. For its potential applications in agriculture and medicine, GHRH analog with higher activity and longer half-life has been looked for. By using the fusion expression with unique acid labile linker Asp-Pro and biochemical purification, the three novel GHRH peptides, Pro-Pro-hGHRH(1–44)-Gly-Gly-Cys, Pro-hGHRH(1–44)-Gly-Gly-Cys, and ¹Pro-GHRH(2–44)-Gly-Gly-Cys, were obtained. The peptide molecular weight with 5,455, 5,373 or 5,210 Da measured by EIS-MS is coincident with the actual values. The peptides at 0.1–10 μg/ml increased rat pituitary GH releases in a dose-dependent manner and at 5 μg/ml increased human pituitary GH releases. The activity comparisons showed that at 10 μg/ml there were significant between ¹Pro-hGHRH(2–44)-Gly-Gly-Cys and Pro-Pro-hGHRH(1–44)-Gly-Gly-Cys or Pro-hGHRH(1–44)-Gly-Gly-Cys, ¹Pro-hGHRH(2–44) (P < 0.05). The ¹Pro-hGHRH(2–44)-Gly-Gly-Cys showed the highest GH release from rat pituitary. The activity results showed that the N-terminal Pro modulations and the C-terminal Gly-Gly-Cys extension regulate GH release from pituitary. The results showed that the three peptides had good GH release, function-selectivity and species specificity.