5-氨基咪唑-4-甲酰胺核糖核苷(AICAr)是AMPK活性的最常用的药理学调节剂之一。大多数早期研究AMPK的作用,在代谢的生理调节和癌症的发病机理中,仅基于使用AICAr作为AMPK激活剂。即使引入了更复杂的AMPK下调和敲除模型,AICAL仍然是许多关注AMPK生物学的研究的常规起点。然而,越来越多的研究表明,许多AICAL效应,以前归因于AMPK激活,实际上是AMPK独立的。这篇综述旨在概述AICAr对代谢的AMPK依赖性和AMPK非依赖性影响的现有知识。缺氧,锻炼,核苷酸合成,和癌症,在理解AMPK信号通路的背景下,在解释基于AICAr的研究时呼吁谨慎。
5-Aminoimidazole-4-carboxamide ribonucleoside (AICAr) has been one of the most commonly used pharmacological modulators of AMPK activity. The majority of early studies on the role of AMPK, both in the physiological regulation of metabolism and in cancer pathogenesis, were based solely on the use of AICAr as an AMPK-activator. Even with more complex models of AMPK downregulation and knockout being introduced, AICAr remained a regular starting point for many studies focusing on AMPK biology. However, there is an increasing number of studies showing that numerous AICAr effects, previously attributed to AMPK activation, are in fact AMPK-independent. This
review aims to give an overview of the present knowledge on AMPK-dependent and AMPK-independent effects of AICAr on metabolism, hypoxia, exercise, nucleotide synthesis, and cancer, calling for caution in the interpretation of AICAr-based studies in the context of understanding AMPK signaling pathway.