The pregnane X receptor in tuberculosis therapeutics.
The pregnane X receptor in tuberculosis therapeutics.
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DOI：
10.1517/17425255.2016.1121381
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发表时间：
2016
影响因子：
4.3
通讯作者：
Ma X
中科院分区：
文献类型：
--
作者：
Shehu AI;Li G;Xie W;Ma X
在传染病中，结核病仍然是仅次于艾滋病毒的第二大死因。结核病治疗需要多种药物的组合，包括利福霉素类。然而，利福霉素是人β-内酰胺酶X受体（PXR）的激活剂，PXR是一种调节药物代谢、耐药性、能量代谢和免疫应答的转录因子。利福霉素介导的PXR激活可能影响结核病治疗的结果。本文综述了PXR在调节抗结核药物代谢、疗效、毒性和耐药性方面的作用，以及PXR的多态性可能影响结核病易感性。除了介导结核病治疗中的药物代谢和毒性外，PXR的广泛功能未得到充分认识，因此未得到充分研究。需要进一步的研究来确定PXR激活对TB治疗结果的总体影响。
Among the infectious diseases, tuberculosis (TB) remains the second cause of death after HIV. TB treatment requires the combination of multiple drugs including the rifamycin class. However, rifamycins are activators of human pregnane X receptor (PXR), a transcription factor that regulates drug metabolism, drug resistance, energy metabolism, and immune response. Rifamycin-mediated PXR activation may affect the outcome of TB therapy. This review describes the role of PXR in modulating metabolism, efficacy, toxicity, and resistance to anti-TB drugs; as well as polymorphisms of PXR that potentially affect TB susceptibility. The wide range of PXR functions aside mediating drug metabolism and toxicity in TB therapy is underappreciated and thus understudied. Further studies are needed to determine the overall impact of PXR activation on the outcome of TB therapy.