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

Efficient microwave-assisted synthesis of human islet amyloid polypeptide designed to facilitate the specific incorporation of labeled amino acids.
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DOI:
10.1021/ol101981b
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发表时间:
2010-11-05
期刊:
影响因子:
5.2
通讯作者:
Raleigh, Daniel P.
Raleigh, Daniel P.
中科院分区:
化学1区
文献类型:
--
作者:
Marek, Peter;Woys, Ann Marie;Sutton, Kelvin;Zanni, Martin T.;Raleigh, Daniel P.

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利用两种假脯氨酸(序列中突出显示为蓝色)与微波技术相结合,开发了一种具有成本效益、缩短时间的淀粉样蛋白生成性37残基胰岛淀粉样多肽(IAPP)固相合成方法。产率是常规合成的两倍。该方案的实用性通过13 C18 O标记的Ser-20 IAPP变体的合成来证明,该变体是通过其他方案标记的极其昂贵且具有化学挑战性的位点。透射电镜分析显示该肽形成正常的淀粉样蛋白。
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 13C18O-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.
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