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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Mitogen-activated protein kinase 4 of Leishmania parasite as a therapeutic target.
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Mitogen-activated protein kinase 4 of Leishmania parasite as a therapeutic target.

机译:利什曼原虫寄生虫的丝裂原活化蛋白激酶4作为治疗靶标。

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摘要

Protein kinases are important regulators of many different cellular processes such as transcriptional control, cell cycle progression and differentiation, and have drawn much attention as potential drug targets. Leishmania mexicana mitogen-activated protein kinase 4 (LmxMPK4) is crucial for the survival of the parasite. As the crystal structure of the enzyme is not known, we have used bioinformatics techniques to model LmxMPK4 structure. The current study reveals conservation of all sequence and structural motifs of LmxMPK4. Study shows mitogen-activated protein kinases are highly conserved throughout different Leishmania species and significant divergence is observed towards mammalian mitogen-activated protein kinases. Additionally, using virtual docking methods, we have identified inhibitors for LmxMPK4. The sequence and structure analysis results were helpful in identifying the ligand binding sites and molecular function of the Leishmania specific mitogen-activated protein kinase.
机译:蛋白激酶是许多不同细胞过程(例如转录控制,细胞周期进程和分化)的重要调节剂,并作为潜在的药物靶标引起了广泛关注。墨西哥利什曼原虫促分裂原活化蛋白激酶4(LmxMPK4)对于寄生虫的生存至关重要。由于该酶的晶体结构未知,我们已使用生物信息学技术对LmxMPK4结构进行建模。当前的研究揭示了LmxMPK4的所有序列和结构基序的保守性。研究表明,在不同的利什曼原虫物种中,丝裂原激活的蛋白激酶高度保守,并且观察到朝向哺乳动物丝裂原激活的蛋白激酶的显着差异。此外,使用虚拟对接方法,我们确定了LmxMPK4抑制剂。序列和结构分析结果有助于鉴定利什曼原虫特异性促分裂原活化蛋白激酶的配体结合位点和分子功能。

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