Gregory R A, Tracy H J, Harris J I, Runswick M J, Moore S, Kenner G W, Ramage R
Hoppe Seylers Z Physiol Chem. 1979 Jan;360(1):73-80. doi: 10.1515/bchm2.1979.360.1.73.
Evidence is presented that minigastrin is the C-terminal tetradecapeptide amide of gastrin and not the tridecapeptide amide as previously reported. Synthesis of the tetradecapeptide amide sequence, Trp-Leu-[Glu]5-Ala-Tyr-Gly-Trp-Met-Asp-Phe-Nh2, was achieved by a series of fragment couplings which were mediated by the dicyclohexylcarbodiimide procedure in presence of either N-hydroxysuccinimide or 1-hydroxybenzotriazole. Purification of all intermediate fragments, and of the final protected tetradecapeptide amide, was by Sephadex LH-20 chromatography. Removal of the protecting groups was effected by treatment with 90% trifluoroacetic acid in the presence of a large excess of scavengers. Purification by ion-exchange chromatography afforded the pure tetradecapeptide amide. This material had full physiological activity.
有证据表明,小胃泌素是胃泌素的C末端十四肽酰胺,而非先前报道的十三肽酰胺。通过一系列片段偶联反应合成了十四肽酰胺序列Trp-Leu-[Glu]5-Ala-Tyr-Gly-Trp-Met-Asp-Phe-Nh2,这些反应由二环己基碳二亚胺法介导,反应过程中存在N-羟基琥珀酰亚胺或1-羟基苯并三唑。所有中间片段以及最终的保护十四肽酰胺均通过Sephadex LH-20色谱法进行纯化。在大量清除剂存在的情况下,用90%的三氟乙酸处理以去除保护基团。通过离子交换色谱法纯化得到纯的十四肽酰胺。该物质具有完全的生理活性。