The Faculty of Health Sciences, Simon Fraser University, 8888 University Drive, Burnaby, BC, Canada.
Curr Mol Med. 2013 Aug;13(7):1047-65. doi: 10.2174/15665240113139990042.
The basic Helix-Loop-Helix/PER-ARNT-SIM (bHLH-PAS) domain family of transcription factors mediates cellular responses to a variety of internal and external stimuli. As functional transcription factors, these proteins act as bHLH-PAS heterodimers and can be further sub-classified into sensory/activated subunits and regulatory or ARNT-like proteins. This class of proteins act as master regulators of the bHLH-PAS superfamily of transcription factors that mediate circadian rhythm gene programs, innate and adaptive immune responses, oxygen-sensing mechanisms and compensate for deleterious environmental exposures. Some contribute to the etiology of human pathologies including cancer because of their effects on cell growth and metabolism. We will review the canonical roles of ARNT and ARNT-like proteins with an emphasis on coactivator selectivity and recruitment. We will also discuss recent advances in our understanding of noncanonical DNA-binding independent or off-target roles of ARNT that are uncoupled from its classic heterodimeric bHLH-PAS binding partners. Understanding the DNA binding-independent functions of ARNT may identify novel therapeutic options for the treatment of a large spectrum of disease states.
基本螺旋-环-螺旋/PER-ARNT-SIM(bHLH-PAS)转录因子家族介导细胞对各种内部和外部刺激的反应。作为功能性转录因子,这些蛋白质作为 bHLH-PAS 异二聚体发挥作用,并且可以进一步细分为感应/激活亚基和调节或 ARNT 样蛋白。该蛋白类作为 bHLH-PAS 转录因子超家族的主要调节剂,介导昼夜节律基因程序、先天和适应性免疫反应、氧感应机制,并补偿有害的环境暴露。由于它们对细胞生长和代谢的影响,一些蛋白导致人类病理学的病因。我们将回顾 ARNT 和 ARNT 样蛋白的典型作用,重点讨论共激活剂的选择性和募集。我们还将讨论我们对 ARNT 的非典型 DNA 结合独立或非靶作用的理解的最新进展,这些作用与其经典的 bHLH-PAS 异二聚体结合伙伴分离。了解 ARNT 的 DNA 结合非依赖性功能可能为治疗大范围的疾病状态确定新的治疗选择。