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:
影响因子:
--
通讯作者:
Hays FA
中科院分区:
文献类型:
--
作者:
Boswell-Casteel RC;Hays FA
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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