平衡核苷转运蛋白(ENT)是介导核苷转运的多位整合膜蛋白,核碱基,和治疗类似物。最佳表征的ENT是人转运蛋白hENT1和hENT2。然而,还研究了非哺乳动物真核ENT(例如,酵母,寄生原生动物)。ENT是负责调节30多种已批准药物的功效的主要药物靶标。然而,ENT介导的底物识别的分子机制和化学决定因素,绑定,抑制,和运输知之甚少。这篇综述通过对遗传学的调查研究,突出了对ENT表征的发现。渗透剂和抑制剂相互作用,诱变,和ENT功能的结构模型。
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.