The antimalarial drugs chloroquine and primaquine inhibit pyridoxal kinase, an essential enzyme for vitamin B6 production
The antimalarial drugs chloroquine and primaquine inhibit pyridoxal kinase, an essential enzyme for vitamin B6 production
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抗疟药氯喹和伯氨喹会抑制吡哆醛激酶（维生素 B6 生成的必需酶）
DOI：
10.1016/j.febslet.2014.08.011
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发表时间：
2014
期刊：
影响因子：
3.5
通讯作者：
Horiuchi H
中科院分区：
文献类型：
--
作者：
Kimura T;Shirakawa R;Yaoita N;Hayashi T;Nagano K;Horiuchi H
氯喹和伯喹等喹啉衍生物被广泛用于治疗疟疾。这些药物还用于治疗锥虫病，最近还用于癌症治疗。然而，这些药物的分子靶点(S)仍不清楚。在这项研究中，我们已经确定人吡哆醛激酶是伯喹的结合蛋白。伯氨喹对疟疾、锥虫和人的吡哆醛酶有抑制作用，而氯喹只抑制疟疾的吡哆醛酶。因此，我们确定吡哆醛激酶是抗疟疾药物氯喹和伯喹的一个可能的靶分子。
Quinoline derivatives such as chloroquine and primaquine are widely used for the treatment of malaria. These drugs are also used for the treatment of trypanosomiasis, and more recently for cancer therapy. However, molecular target(s) of these drugs remain unclear. In this study, we have identified human pyridoxal kinase as a binding protein of primaquine. Primaquine inhibited pyridoxal kinases of malaria, trypanosome and human, while chloroquine inhibited only malaria pyridoxal kinase. Thus, we have identified pyridoxal kinase as a possible target molecule of the antimalarial drugs chloroquine and primaquine.