Department of Biochemistry, Duke University Medical Center, 303 Research Drive, Durham, NC, 27710, USA. Electronic address: https://twitter.com/@nick_rite.
Department of Biochemistry, Duke University Medical Center, 303 Research Drive, Durham, NC, 27710, USA.
Curr Opin Struct Biol. 2022 Jun;74:102378. doi: 10.1016/j.sbi.2022.102378. Epub 2022 Apr 26.
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 introduce 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.
溶质载体（SLCs）是一类膜转运蛋白，负责介导亲水分子穿过脂质双分子层。尽管 SLCs 在人类生物学的各个方面都发挥了广泛的作用，但作为治疗靶点，它们的研究还远远不够。在这篇简短的综述中，我们首先讨论了一些通过抑制人类 SLCs 发挥作用的药物的成功案例，并介绍了一些具有未开发治疗潜力的人类 SLCs 的例子。然后，我们重点介绍了两项最近的结构研究，这些研究揭示了针对两种具有临床相关性的不同人类主要促进因子超家族（MFS）转运蛋白的抑制作用的详细结构机制。
