Synthetic transporters for sulfate: a new method for the direct detection of lipid bilayer sulfate transport
Synthetic transporters for sulfate: a new method for the direct detection of lipid bilayer sulfate transport
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DOI：
10.1039/c3sc52006d
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发表时间：
2014-03-01
期刊：
影响因子：
8.4
通讯作者：
Gale, Philip A.
中科院分区：
文献类型：
--
作者：
Busschaert, Nathalie;Karagiannidis, Louise E.;Gale, Philip A.
合成小分子对阴离子的跨膜转运是超分子化学中一个不断发展的领域，主要集中在氯离子的跨膜转运上。另一方面，高度亲水性的硫酸根阴离子跨脂质双层的转运还不太发达，尽管不能跨细胞膜转运硫酸根与多种遗传疾病有关。三硫脲具有高硫酸盐亲和力，并且已被证明是优异的氯化物和碳酸氢盐转运体。本文报道了一系列基于三（2-氨基乙基）胺或环肽支架的三脲和三硫脲的硫酸盐转运能力。我们开发了一种基于S-33 NMR的新技术，该技术可用于监测硫酸盐转运，使用S-33标记的硫酸盐和顺磁剂如Mn 2+和Fe 3+来区分囊内和囊外硫酸盐。合理的硫酸盐转运能力，发现报告的三-脲和三-硫脲，提供了一个起点，更强大的合成硫酸盐转运蛋白，可用于治疗某些通道病或作为生物硫酸盐转运蛋白的模型的发展。
The transmembrane transport of anions by small synthetic molecules is a growing field in supramolecular chemistry and has focussed mainly on the transmembrane transport of chloride. On the other hand, the transport of the highly hydrophilic sulfate anion across lipid bilayers is much less developed, even though the inability to transport sulfate across cellular membranes has been linked to a variety of genetic diseases. Tris-thioureas possess high sulfate affinities and have been shown to be excellent chloride and bicarbonate transporters. Herein we report the sulfate transport abilities of a series of tris-ureas and tris-thioureas based on a tris(2-aminoethyl)amine or cyclopeptide scaffold, We have developed a new technique based on S-33 NMR that can be used to monitor sulfate transport, using S-33-labelled sulfate and paramagnetic agents such as Mn2+ and Fe3+ to discriminate between intra- and extravesicular sulfate. Reasonable sulfate transport abilities were found for the reported tris-ureas and tris-thioureas, providing a starting point for the development of more powerful synthetic sulfate transporters that can be used in the treatment of certain channelopathies or as a model for biological sulfate transporters.