Abstract Protein drugs are attracting increasing attention. Eight of best-selling drugs in worldwide are proteins. Crystallization is an important protein purification method; however, it remains a bottleneck step. Heterogeneous nucleate is an effective method of enhancing protein crystallization. Cyclodextrin has been widely used in pharmaceutics, and our previous study showed that it is an effective heterogeneous nucleate for enhancing protein crystallization, and it may be widely used in purification of protein drugs. However, cyclodextrin must be added into the crystallization plate wells by hand, which is labor intensive and is not beneficial to automated crystallization screening. We grafted β-cyclodextrin (β-CD) and its derivatives (i.e., p-toluenesulfonyl-β-cyclodextrin [PTCD], mono-(6-(1,6-hexamethylenediamine)-6-deoxy)-β-cyclodextrin [MHCD] and mercapto-β-cyclodextrin [MCD]) on crystallization plates and tested their effects on protein crystallization. Protein crystallization success rate was improved, particularly for the PTCD-grafted group. This is an easy method to facilitate protein crystallization and can be widely applied for automatic crystallization screening.

中文翻译：

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环糊精及其衍生物通过接枝在结晶板上增强蛋白质结晶

摘要 蛋白质药物越来越受到关注。世界上最畅销的药物中有八种是蛋白质。结晶是一种重要的蛋白质纯化方法；然而，这仍然是一个瓶颈步骤。异质成核是增强蛋白质结晶的有效方法。环糊精已广泛应用于制药，我们之前的研究表明，它是一种有效的促进蛋白质结晶的异质成核物质，可广泛用于蛋白质药物的纯化。但是，环糊精必须手工加入结晶板孔中，劳动强度大，不利于自动结晶筛选。我们接枝了 β-环糊精 (β-CD) 及其衍生物（即对甲苯磺酰基-β-环糊精 [PTCD]、单-(6-(1, 6-六亚甲基二胺)-6-脱氧)-β-环糊精 [MHCD] 和巯基-β-环糊精 [MCD]) 在结晶板上并测试它们对蛋白质结晶的影响。蛋白质结晶成功率得到提高，特别是对于 PTCD 接枝组。这是一种促进蛋白质结晶的简便方法，可广泛应用于自动结晶筛选。