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双组分及磷酸化信号转导系统作为治疗靶点。

Two-component and phosphorelay signal-transduction systems as therapeutic targets.

作者信息

Stephenson Keith, Hoch James A

机构信息

Department of Molecular and Experimental Medicine, MEM-116, The Scripps Research Institute, La Jolla, California 92037, USA.

出版信息

Curr Opin Pharmacol. 2002 Oct;2(5):507-12. doi: 10.1016/s1471-4892(02)00194-7.

Abstract

Two-component and phosphorelay signal-transduction systems of pathogenic bacteria control the expression of genes encoding virulence factors and essential functions. Recent systematic gene inactivation studies have confirmed the integral role of two-component systems in the pathogenesis of diseases caused by several microorganisms and highlighted the validity of using these systems as targets for therapeutic intervention. Structural studies of signal-transduction proteins have recently revealed common features that may allow rational drug design for therapeutic intervention. In particular, the conserved domains of response regulators may represent the best targets for inhibition.

摘要

病原菌的双组分和磷酸化信号转导系统控制着编码毒力因子和基本功能的基因的表达。最近的系统基因失活研究证实了双组分系统在几种微生物引起的疾病发病机制中的不可或缺的作用,并突出了将这些系统用作治疗干预靶点的有效性。信号转导蛋白的结构研究最近揭示了一些共同特征,这可能有助于进行合理的药物设计以用于治疗干预。特别是,应答调节因子的保守结构域可能是抑制的最佳靶点。

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