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高效微波辅助合成人胰岛淀粉样多肽,旨在促进标记氨基酸的特异性掺入。

Efficient microwave-assisted synthesis of human islet amyloid polypeptide designed to facilitate the specific incorporation of labeled amino acids.

机构信息

Department of Chemistry, State University of New York at Stony Brook, Stony Brook, New York 11794-3400, United States.

出版信息

Org Lett. 2010 Nov 5;12(21):4848-51. doi: 10.1021/ol101981b.

DOI:10.1021/ol101981b
PMID:20931985
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3052696/
Abstract

A cost-efficient, time-reducing solid-phase synthesis of the amyloidogenic, 37 residue islet amyloid polypeptide (IAPP) is developed using two pseudoprolines (highlighted blue in sequence) in combination with microwave technology. A yield twice that obtained with conventional syntheses is realized. The utility of this protocol is demonstrated by the synthesis of a (13)C(18)O-labeled Ser-20 IAPP variant, a prohibitively expensive and chemically challenging site to label via other protocols. TEM analysis shows the peptide forms normal amyloid (abstract image).

摘要

采用两种假脯氨酸(序列中用蓝色突出显示)结合微波技术,开发出了一种具有成本效益、耗时短的 37 残基胰岛淀粉样多肽(IAPP)的固相合成方法。与常规合成方法相比,产率提高了一倍。通过合成(13)C(18)O 标记的 Ser-20 IAPP 变体,证明了该方案的实用性,通过其他方案标记这个位置既昂贵又具有化学挑战性。TEM 分析显示该肽形成正常的淀粉样纤维(抽象图像)。

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J Mol Biol. 2010 Jul 23;400(4):878-88. doi: 10.1016/j.jmb.2010.05.041. Epub 2010 Jun 1.
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Direct solid-phase synthesis of the beta-amyloid (1-42) peptide using controlled microwave heating.采用控温微波加热直接固相合成β-淀粉样肽(1-42)。
J Org Chem. 2010 Mar 19;75(6):2103-6. doi: 10.1021/jo100136r.
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Microwave assisted SPPS of amylin and its toxicity of the pure product to RIN-5F cells.采用微波辅助固相合成法合成的胰岛淀粉样多肽及其对 RIN-5F 细胞的毒性纯品。
Biopolymers. 2010;94(3):323-30. doi: 10.1002/bip.21370.
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