Recent advances on the inhibition of human solute carriers: Therapeutic implications and mechanistic insights.

Recent advances on the inhibition of human solute carriers: Therapeutic implications and mechanistic insights.
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DOI:
10.1016/j.sbi.2022.102378
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发表时间:
2022-06
影响因子:
6.8
通讯作者:
Lee, Seok-Yong
Lee, Seok-Yong
中科院分区:
生物学2区
文献类型:
--
作者:
Wright, Nicholas J.;Lee, Seok-Yong

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溶质载体(SLC)是膜转运蛋白,其任务是介导亲水性分子穿过脂质双层。尽管SLC在人类生物学的各个方面都发挥着广泛的作用,但其作为治疗靶点的研究仍然远远不足。在这篇简短的综述中,我们首先讨论了一些成功的药物案例,这些药物通过抑制人类SLC发挥其作用机制,并选择了具有未开发治疗潜力的人类SLC的例子。然后,我们强调了最近的两个结构研究,揭示了详细的结构机制的抑制表现出对两个不同的人类主要易化超家族(MFS)转运蛋白的临床相关性。
Solute carriers (SLCs) are membrane transport proteins tasked with mediating passage of hydrophilic molecules across lipid bilayers. Despite the extensive roles played in all aspects of human biology, SLCs remain vastly under-explored as therapeutic targets. In this brief review, we first discuss a few successful cases of drugs that exert their mechanisms of action through inhibition of human SLCs and select examples of human SLCs that have untapped therapeutic potential. We then highlight two recent structural studies which uncovered detailed structural mechanisms of inhibition exhibited against two different human major facilitator superfamily (MFS) transporters of clinical relevance.
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