Screening and classifying small-molecule inhibitors of amyloid formation using ion mobility spectrometry-mass spectrometry.
Screening and classifying small-molecule inhibitors of amyloid formation using ion mobility spectrometry-mass spectrometry.
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搜索与淀粉样蛋白的构象和淀粉样蛋白组合的抑制是一个重要的挑战，因为许多蛋白质的蛋白质的蛋白质是抑制均可用各种机制，因此抑制淀粉样蛋白的挑战是一个重要的挑战。 Throughput method based on ion mobility spectrometry-mass spectrometry (IMS-MS) that is capable of rapidly detecting small molecules that bind to amyloid precursors, identifying the interacting protein species, and defining the mode of inhibition. Using this method we have classified a variety of small molecules that are potential inhibitors of human islet amyloid polypeptide (hIAPP) aggregation or amyloid-beta 1-40 (Aβ40) aggregation as either specific,非特异性，菌落或非相互作用。
The search for therapeutic agents which bind specifically to precursor protein conformations and inhibit amyloid assembly is an important challenge. Identifying such inhibitors is difficult since many protein precursors of aggregation are partially folded or intrinsically disordered, ruling out structure-based design. Furthermore, inhibitors can act by a variety of mechanisms, including specific or non-specific binding, as well as colloidal inhibition. Here we report a high throughput method based on ion mobility spectrometry-mass spectrometry (IMS-MS) that is capable of rapidly detecting small molecules that bind to amyloid precursors, identifying the interacting protein species, and defining the mode of inhibition. Using this method we have classified a variety of small molecules that are potential inhibitors of human islet amyloid polypeptide (hIAPP) aggregation or amyloid-beta 1-40 (Aβ40) aggregation as either specific, non-specific, colloidal or non-interacting. We also demonstrate the ability of IMS-MS to screen for inhibitory small molecules in a 96-well plate format and use this to discover a new inhibitor of hIAPP amyloid assembly.
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影响因子：
5.6
作者：
Meng F;Raleigh DP
通讯作者：
Raleigh DP
影响因子：
5.2
作者：
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通讯作者：
Raleigh, Daniel P.
影响因子：
5.6
作者：
Meng F;Abedini A;Plesner A;Middleton CT;Potter KJ;Zanni MT;Verchere CB;Raleigh DP
通讯作者：
Raleigh DP
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DOI：
10.1016/j.bbrc.2012.02.042
发表时间：
2012-03-16
影响因子：
3.1
作者：
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通讯作者：
Huang, Kun
DOI：
10.1152/ajpendo.00082.2006
发表时间：
2006-12-01
影响因子：
5.1
作者：
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通讯作者：
Butler, Peter C.