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通过混合酸酐法合成血管活性肠肽(VIP)。

Synthesis of vasoactive intestinal peptide (VIP) via the mixed anhydride method.

作者信息

Schaaper W M, Beyerman H C

出版信息

Peptides. 1984 Mar-Apr;5(2):167-8. doi: 10.1016/0196-9781(84)90201-8.

Abstract

Porcine VIP was synthesized from three segments. The segments, VIP(1-6), VIP(7-13), and VIP(14-28), were synthesized via the Repetitive Excess Mixed Anhydride (REMA) method. The low solubility of the C-terminal segment was greatly improved by a temporary substitution of Asn28 by a beta-t-butyl aspartic acid ester. The segments VIP(1-6) and VIP(7-13) were purified by HPLC and coupled via the mixed anhydride method. The product was purified by gel filtration. VIP was synthesized from VIP(1-13) and VIP(14-28) by the same procedure. After deprotection, Met17-sulfoxide reduction, and purification by ion-exchange chromatography, the product was found to have the expected amino acid composition and biological potency. A HPLC purified sample was compared with several commercial preparations of varying purity.

摘要

猪血管活性肠肽(Porcine VIP)由三个片段合成。这三个片段,即VIP(1 - 6)、VIP(7 - 13)和VIP(14 - 28),通过重复过量混合酸酐(REMA)法合成。通过用β-叔丁基天冬氨酸酯暂时取代Asn28,大大提高了C末端片段的低溶解性。片段VIP(1 - 6)和VIP(7 - 13)通过高效液相色谱(HPLC)纯化,并通过混合酸酐法偶联。产物通过凝胶过滤纯化。通过相同程序由VIP(1 - 13)和VIP(14 - 28)合成了VIP。脱保护、Met17-亚砜还原以及离子交换色谱纯化后,发现产物具有预期的氨基酸组成和生物活性。将一个HPLC纯化的样品与几种不同纯度的商业制剂进行了比较。

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Solid-phase synthesis of porcine vasoactive intestinal peptide.
Int J Pept Protein Res. 1980 Jan;15(1):73-8. doi: 10.1111/j.1399-3011.1980.tb02552.x.

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