Berdeaux Rebecca, Hutchins Chase
Department of Integrative Biology and Pharmacology, Center for Metabolic and Degenerative Diseases, The Brown Foundation Institute of Molecular Medicine, McGovern Medical School, University of Texas Health Science Center Houston, Houston, TX, United States.
Graduate Program in Biochemistry and Cell Biology, The MD Anderson-UTHealth Graduate School of Biomedical Sciences, Houston, TX, United States.
Front Endocrinol (Lausanne). 2019 Aug 2;10:535. doi: 10.3389/fendo.2019.00535. eCollection 2019.
cAMP is one of the earliest described mediators of hormone action in response to physiologic stress that allows acute stress responses and adaptation in every tissue. The classic role of cAMP signaling in metabolic tissues is to regulate nutrient partitioning. In response to acute stress, such as epinephrine released during strenuous exercise or fasting, intramuscular cAMP liberates glucose from glycogen and fatty acids from triglycerides. In the long-term, activation of Gs-coupled GPCRs stimulates muscle growth (hypertrophy) and metabolic adaptation through multiple pathways that culminate in a net increase of protein synthesis, mitochondrial biogenesis, and improved metabolic efficiency. This review focuses on regulation, function, and transcriptional targets of CREB (cAMP response element binding protein) and CRTCs (CREB regulated transcriptional coactivators) in skeletal muscle and the potential for targeting this pathway to sustain muscle mass and metabolic function in type 2 diabetes and cancer. Although the muscle-autonomous roles of these proteins might render them excellent targets for both conditions, pharmacologic targeting must be approached with caution. Gain of CREB-CRTC function is associated with excess liver glucose output in type 2 diabetes, and growing evidence implicates CREB-CRTC activation in proliferation and invasion of different types of cancer cells. We conclude that deeper investigation to identify skeletal muscle specific regulatory mechanisms that govern CREB-CRTC transcriptional activity is needed to safely take advantage of their potent effects to invigorate skeletal muscle to potentially improve health in people with type 2 diabetes and cancer.
环磷酸腺苷(cAMP)是最早被描述的、在生理应激反应中发挥激素作用的介质之一,它能使每个组织产生急性应激反应并实现适应性变化。cAMP信号在代谢组织中的经典作用是调节营养分配。在急性应激反应中,比如剧烈运动或禁食期间释放的肾上腺素,肌肉内的cAMP会促使糖原释放葡萄糖,使甘油三酯释放脂肪酸。从长期来看,Gs偶联的G蛋白偶联受体(GPCRs)的激活会通过多种途径刺激肌肉生长(肥大)和代谢适应,最终导致蛋白质合成、线粒体生物发生的净增加以及代谢效率的提高。本综述聚焦于环磷腺苷效应元件结合蛋白(CREB)和CREB调节的转录共激活因子(CRTCs)在骨骼肌中的调控、功能及转录靶点,以及针对该信号通路以维持2型糖尿病和癌症患者肌肉量和代谢功能的潜力。尽管这些蛋白质在肌肉中的自主作用可能使它们成为这两种疾病的理想靶点,但药物靶向治疗必须谨慎进行。CREB-CRTC功能增强与2型糖尿病患者肝脏葡萄糖输出过多有关,越来越多的证据表明CREB-CRTC激活与不同类型癌细胞的增殖和侵袭有关。我们得出结论,需要进行更深入的研究,以确定控制CREB-CRTC转录活性的骨骼肌特异性调节机制,从而安全地利用它们的强大作用来增强骨骼肌功能,有可能改善2型糖尿病和癌症患者的健康状况。