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首页> 外文期刊>Chemistry: A European journal >Tilting and Tumbling in Transmembrane Anion Carriers: Activity Tuning through n-Alkyl Substitution
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Tilting and Tumbling in Transmembrane Anion Carriers: Activity Tuning through n-Alkyl Substitution

机译：跨膜阴离子载体中的倾斜和翻转：通过正烷基取代进行的活性调节

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摘要

Anion transport by synthetic carriers (anionophores) holds promise for medical applications, especially the treatment of cystic fibrosis. Among the factors which determine carrier activity, the size and disposition of alkyl groups is proving remarkably important. Herein we describe a series of dithioureidodecalin anionophores, in which alkyl substituents on one face are varied from C-0 to C-10 in two-carbon steps. Activities increase then decrease as the chain length grows, peaking quite sharply at C-6. Molecular dynamics simulations showed the transporter chloride complexes releasing chloride as they approach the membrane-aqueous interface. The free transporter then stays at the interface, adopting an orientation that depends on the alkyl substituent. If chloride release is prevented, the complex is positioned similarly. Longer chains tilt the binding site away from the interface, potentially freeing the transporter or complex to move through the membrane. However, chains which are too long can also slow transport by inhibiting movement, and especially reorientation, within the phospholipid bilayer.
机译：合成载体（阴离子载体）对阴离子的运输在医学上尤其是在治疗囊性纤维化方面具有广阔的前景。在决定载体活性的因素中，烷基的大小和位置被证明非常重要。在这里，我们描述了一系列的二硫脲基十氢化萘阴离子载体，其中一个表面上的烷基取代基在两个碳原子的步骤中从C-0变为C-10。活性随着链长的增加而增加，然后减少，在C-6处达到最高峰。分子动力学模拟表明，转运蛋白氯化物配合物在接近膜-水界面时释放出氯化物。然后，自由转运蛋白停留在界面上，采用取决于烷基取代基的取向。如果防止氯化物释放，则将络合物放置在类似位置。较长的链使结合位点远离界面倾斜，从而有可能释放转运蛋白或复合物以穿过膜。但是，太长的链也会通过抑制磷脂双层内的运动，特别是重新取向而减慢运输速度。

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