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精氨酸激酶:锥虫病的一个潜在药理学靶点。

Arginine kinase: a potential pharmacological target in trypanosomiasis.

作者信息

Pereira Claudio A

机构信息

IDIM, Combatientes de Malvinas 3150, (1427) Bs. As., Argentina.

出版信息

Infect Disord Drug Targets. 2014;14(1):30-6. doi: 10.2174/1871526514666140713144103.

Abstract

Trypanosomatids parasites have complex life cycles which involve a wide diversity of milieus with very different physicochemical properties. Arginine kinase is one of the key enzymes, responsible for the parasites' metabolic plasticity, which maintains the cell energy homeostasis during environment changes. Arginine kinase catalyzes the reversible phosphorylation between phosphoarginine and ADP. The phosphagen phosphoarginine sustains high levels of cellular activity until metabolic events, such as glycolysis and oxidative phosphorylation, are switched on. In different unicellular and multicellular organisms including trypanosomatids, it was demonstrated that arginine kinase is an important component in resistance mechanisms to different stress factors, such as reactive oxygen species, trypanocidal drugs, pH and starvation. In addition, few arginine kinase inhibitors were identified during the lasts years, some of them with trypanocidal activity, such as polyphenolic compounds. All these unique features, in addition to the fact that arginine kinase is completely absent in mammals, make this pathway a favorable start point for rational drug design for the treatment of human trypanosomamiases.

摘要

锥虫类寄生虫具有复杂的生命周期,涉及多种具有截然不同物理化学性质的环境。精氨酸激酶是关键酶之一,负责寄生虫的代谢可塑性,在环境变化期间维持细胞能量稳态。精氨酸激酶催化磷酸精氨酸和ADP之间的可逆磷酸化反应。磷酸原磷酸精氨酸维持高水平的细胞活性,直到糖酵解和氧化磷酸化等代谢过程开启。在包括锥虫类在内的不同单细胞和多细胞生物中,已证明精氨酸激酶是对不同应激因素(如活性氧、杀锥虫药物、pH值和饥饿)的抗性机制中的重要组成部分。此外,在过去几年中鉴定出了少数精氨酸激酶抑制剂,其中一些具有杀锥虫活性,如多酚类化合物。除了哺乳动物中完全不存在精氨酸激酶这一事实外,所有这些独特特性使该途径成为用于治疗人类锥虫病的合理药物设计的有利起点。

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