Unidad de Biología Molecular, Institut Pasteur de Montevideo, Mataojo 2020, Montevideo 11400, Uruguay.
Grupo de Química Medicinal, Laboratorio de Química Orgánica, Facultad de Ciencias-Facultad de Química, Universidad de la República, Iguá 4225, Montevideo 11400, Uruguay.
Exp Parasitol. 2014 May;140:33-8. doi: 10.1016/j.exppara.2014.03.013. Epub 2014 Mar 13.
Benznidazole (Bzn) is a nitroimidazole drug currently used as first line treatment against Chagas disease, a neglected tropical disease caused by the flagellated protozoan Trypanosoma cruzi. Although the drug has been used since the late 1960s, its mechanism of action is not fully understood. In an attempt to study Bzn mode of action, a structurally modified derivative of the drug was synthesized and immobilized into a solid matrix. This allowed enrichment of T. cruzi proteins capable of binding immobilized Bzn, which were subsequently analysed by mass spectrometry. The proteins identified as specific non-covalent Bzn interactors were a homologue of the bacterial YjeF proteins, a Sec23A orthologue and the aldo-ketoreductase family member TcAKR. TcAKR is closely related to other enzymes previously associated with Bzn reductive activation such as NTRI and TcOYE. Thus, our untargeted search for Bzn binding partners allowed us to encounter proteins that could be related to drug reductive activation and/or resistance mechanisms.
苯唑硝唑(Bzn)是一种硝基咪唑类药物,目前被用作治疗恰加斯病(一种由鞭毛原生动物克氏锥虫引起的被忽视的热带病)的一线药物。尽管该药物自 20 世纪 60 年代末以来就已被使用,但它的作用机制仍不完全清楚。为了研究 Bzn 的作用机制,合成了该药物的结构修饰衍生物,并将其固定在固体基质上。这使得能够富集能够与固定化 Bzn 结合的 T. cruzi 蛋白,随后通过质谱分析对其进行分析。被鉴定为特定非共价 Bzn 相互作用体的蛋白质是细菌 YjeF 蛋白的同源物、Sec23A 同源物和醛酮还原酶家族成员 TcAKR。TcAKR 与其他先前与 Bzn 还原活化相关的酶(如 NTRI 和 TcOYE)密切相关。因此,我们对 Bzn 结合伴侣的非靶向搜索使我们遇到了可能与药物还原活化和/或耐药机制相关的蛋白质。