A modular approach to triazole-containing chemical inducers of dimerisation for yeast three-hybrid screening.
A modular approach to triazole-containing chemical inducers of dimerisation for yeast three-hybrid screening.
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DOI：
10.3390/molecules180911639
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发表时间：
2013-09-23
期刊：
影响因子：
--
通讯作者：
Westwood NJ
中科院分区：
文献类型：
--
作者：
Tran F;Odell AV;Ward GE;Westwood NJ
酵母三杂交（Y3H）方法在公正地鉴定新型小分子-蛋白质相互作用方面显示出巨大的前景。近年来，它已成功用于将许多生物活性分子与新型蛋白质结合伙伴连接起来。然而，尽管 Y3H 技术作为蛋白质靶标识别方法具有潜在的重要性，但尚未得到广泛采用，部分原因是与复杂的二聚化化学诱导剂 (CID) 的合成相关的挑战。使用潜在的“现成”合成成分开发了一种模块化方法，并允许合成四个含三唑的 CID，MTX-Cmpd2.2-2.5。然后使用 Y3H 方法将这些 CID 与其中三个 CID 进行比较，其中三个 CID 与化合物 2 的已知靶标 TgCDPK1 具有强烈的正相互作用。这些结果表明，我们的合成策略的模块化性质可能有助于克服目前 CID 合成遇到的挑战，并应有助于 Y3H 方法充分发挥其作为无偏见目标识别策略的潜力。
The yeast three-hybrid (Y3H) approach shows considerable promise for the unbiased identification of novel small molecule-protein interactions. In recent years, it has been successfully used to link a number of bioactive molecules to novel protein binding partners. However despite its potential importance as a protein target identification method, the Y3H technique has not yet been widely adopted, in part due to the challenges associated with the synthesis of the complex chemical inducers of dimerisation (CIDs). The development of a modular approach using potentially “off the shelf” synthetic components was achieved and allowed the synthesis of a family of four triazole-containing CIDs, MTX-Cmpd2.2-2.5. These CIDs were then compared using the Y3H approach with three of them giving a strong positive interaction with a known target of compound 2, TgCDPK1. These results showed that the modular nature of our synthetic strategy may help to overcome the challenges currently encountered with CID synthesis and should contribute to the Y3H approach reaching its full potential as an unbiased target identification strategy.
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影响因子：
5.8
作者：
Henthorn, DC;Jaxa-Chamiec, AA;Meldrum, E
通讯作者：
Meldrum, E
影响因子：
2.9
作者：
de Felipe, KS;Carter, BT;Cornish, VW
通讯作者：
Cornish, VW
影响因子：
14.8
作者：
Chidley, Christopher;Haruki, Hirohito;Johnsson, Kai
通讯作者：
Johnsson, Kai
影响因子：
15
作者：
Lin, HN;Abida, WM;Cornish, VW
通讯作者：
Cornish, VW
DOI：
10.1073/pnas.94.20.10618
发表时间：
1997-09-30
影响因子：
11.1
作者：
Amara, JF;Clackson, T;Gilman, M
通讯作者：
Gilman, M