Center for Molecular Studies of the Cell, Faculty of Chemical and Pharmaceutical Sciences/Faculty of Medicine, University of Chile, Santiago, Chile.
Mini Rev Med Chem. 2011 May;11(5):390-8. doi: 10.2174/138955711795445880.
Increasing evidence suggests that nongenomic effects of testosterone and anabolic androgenic steroids (AAS) operate concertedly with genomic effects. Classically, these responses have been viewed as separate and independent processes, primarily because nongenomic responses are faster and appear to be mediated by membrane androgen receptors, whereas long-term genomic effects are mediated through cytosolic androgen receptors regulating transcriptional activity. Numerous studies have demonstrated increases in intracellular Ca2+ in response to AAS. These Ca2+ mediated responses have been seen in a diversity of cell types, including osteoblasts, platelets, skeletal muscle cells, cardiac myocytes and neurons. The versatility of Ca2+ as a second messenger provides these responses with a vast number of pathophysiological implications. In cardiac cells, testosterone elicits voltage-dependent Ca2+ oscillations and IP3R-mediated Ca2+ release from internal stores, leading to activation of MAPK and mTOR signaling that promotes cardiac hypertrophy. In neurons, depending upon concentration, testosterone can provoke either physiological Ca2+ oscillations, essential for synaptic plasticity, or sustained, pathological Ca2+ transients that lead to neuronal apoptosis. We propose therefore, that Ca2+ acts as an important point of crosstalk between nongenomic and genomic AAS signaling, representing a central regulator that bridges these previously thought to be divergent responses.
越来越多的证据表明,睾酮和合成代谢雄激素类固醇(AAS)的非基因组效应与基因组效应协同作用。传统上,这些反应被视为单独和独立的过程,主要是因为非基因组反应更快,似乎是由膜雄激素受体介导的,而长期的基因组效应是通过调节转录活性的细胞质雄激素受体介导的。许多研究已经证明 AAS 会引起细胞内 Ca2+的增加。这些 Ca2+介导的反应已经在多种细胞类型中观察到,包括成骨细胞、血小板、骨骼肌细胞、心肌细胞和神经元。Ca2+作为第二信使的多功能性为这些反应提供了大量的病理生理学意义。在心肌细胞中,睾酮引发电压依赖性 Ca2+振荡和 IP3R 介导的内质网 Ca2+释放,导致 MAPK 和 mTOR 信号的激活,从而促进心肌肥大。在神经元中,根据浓度的不同,睾酮可以引发生理 Ca2+振荡,这对于突触可塑性是必需的,或者引发持续的、病理性的 Ca2+瞬变,导致神经元凋亡。因此,我们提出 Ca2+作为非基因组和基因组 AAS 信号之间的重要交叉点,代表了连接这些先前认为是不同反应的中央调节剂。