Equilibrative nucleoside transporters-A review.

Equilibrative nucleoside transporters-A review.
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DOI:
10.1080/15257770.2016.1210805
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发表时间:
2017-01-02
期刊:
Nucleosides, nucleotides & nucleic acids
影响因子:
--
通讯作者:
Hays FA
Hays FA
中科院分区:
其他
文献类型:
--
作者:
Boswell-Casteel RC;Hays FA

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平衡核苷转运蛋白(ENTs)是一种多位整合膜蛋白,介导核苷、核碱基和治疗类似物的转运。最具特征的ENT是人类转运蛋白hENT1和hENT2。然而,也已经研究了非哺乳动物真核ENT(例如,酵母、寄生原生动物)。ENT是主要的药物靶点,负责调节30多种已批准药物的疗效。然而,ENT介导的底物识别,结合,抑制和运输的分子机制和化学决定因素知之甚少。这篇综述强调了调查研究的遗传学,渗透剂和抑制剂的相互作用,诱变,和结构模型的ENT功能的ENT表征的结果。
Equilibrative nucleoside transporters (ENTs) are polytopic integral membrane proteins that mediate the transport of nucleosides, nucleobases, and therapeutic analogs. The best-characterized ENTs are the human transporters hENT1 and hENT2. However, non-mammalian eukaryotic ENTs have also been studied (e.g., yeast, parasitic protozoa). ENTs are major pharmaceutical targets responsible for modulating the efficacy of more than 30 approved drugs. However, the molecular mechanisms and chemical determinants of ENT-mediated substrate recognition, binding, inhibition, and transport are poorly understood. This review highlights findings on the characterization of ENTs by surveying studies on genetics, permeant and inhibitor interactions, mutagenesis, and structural models of ENT function.
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