Protein Phosphorylation (PHOS) laboratory, Université catholique de Louvain and de Duve Institute, Avenue Hippocrate 75, B-1200 Brussels, Belgium.
Essays Biochem. 2024 Nov 18;68(3):283-294. doi: 10.1042/EBC20240009.
AMP-activated protein kinase (AMPK) is a key regulator of metabolism and a recognised target for the treatment of metabolic diseases such as Type 2 diabetes (T2D). Here, we review how mass spectrometry (MS) can be used to study short-term control by AMPK via protein phosphorylation and long-term control due to changes in protein expression. We discuss how MS can quantify AMPK subunit levels in tissues from different species. We propose hydrogen-deuterium exchange (HDX)-MS to investigate molecular mechanisms of AMPK activation and thermoproteomic profiling (TPP) to assess off-target effects of pharmacological AMPK activators/inhibitors. Lastly, because large MS data sets are generated, we consider different approaches that can be used for their interpretation.
腺苷酸活化蛋白激酶(AMPK)是代谢的关键调节剂,也是治疗 2 型糖尿病(T2D)等代谢疾病的公认靶点。在这里,我们综述了质谱(MS)如何用于研究 AMPK 通过蛋白磷酸化的短期调控和由于蛋白表达变化的长期调控。我们讨论了 MS 如何定量不同物种组织中的 AMPK 亚基水平。我们提出氢氘交换(HDX)-MS 来研究 AMPK 激活的分子机制和热蛋白质组学分析(TPP)来评估药理 AMPK 激活剂/抑制剂的脱靶效应。最后,由于生成了大型 MS 数据集,我们考虑了可用于解释这些数据集的不同方法。