Groeger Alison L, Freeman Bruce A
Department of Pharmacology & Chemical Biology, University of Pittsburgh, PA 15261, USA.
Mol Interv. 2010 Feb;10(1):39-50. doi: 10.1124/mi.10.1.7.
Over the past several years, research on biologically relevant electrophiles has been replete with new insights, expanding our understanding of the roles electrophiles play in vivo. Importantly, many electrophiles can form reversible covalent adducts with both proteins and small-molecule thiols in cells. This post-translational protein modification has important ramifications, including changes in protein enzymatic activity, the transduction of signals within and between cells, and alterations in gene expression. Electrophiles modulate a variety of cellular signaling processes that are involved in several major diseases with inflammatory components. The electrophilic fatty-acid derivatives discussed in this work are naturally occurring products of redox reactions and enzymatic activity. Furthermore, several of these electrophilic species and their derivatives represent potential therapeutic candidates.
在过去几年中，对具有生物学相关性的亲电试剂的研究充满了新的见解，扩展了我们对亲电试剂在体内所起作用的理解。重要的是，许多亲电试剂可与细胞中的蛋白质和小分子硫醇形成可逆的共价加合物。这种翻译后蛋白质修饰具有重要影响，包括蛋白质酶活性的变化、细胞内和细胞间信号的转导以及基因表达的改变。亲电试剂调节多种细胞信号传导过程，这些过程涉及几种具有炎症成分的主要疾病。本文讨论的亲电脂肪酸衍生物是氧化还原反应和酶活性的天然产物。此外，这些亲电物质及其衍生物中的几种代表了潜在的治疗候选物。
