Department of Chemistry, State University of New York at Stony Brook, Stony Brook, New York 11794-3400, United States.
Org Lett. 2010 Nov 5;12(21):4848-51. doi: 10.1021/ol101981b.
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).
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)。