Elies Jacobo, Scragg Jason L, Boyle John P, Gamper Nikita, Peers Chris
Faculty of Medicine and Health, University of Leeds, Leeds, UK.
Faculty of Biological Sciences, School of Biomedical Sciences, University of Leeds, Leeds, UK.
J Physiol. 2016 Aug 1;594(15):4119-29. doi: 10.1113/JP270963. Epub 2016 Feb 25.
Ion channels represent a large and growing family of target proteins regulated by gasotransmitters such as nitric oxide, carbon monoxide and, as described more recently, hydrogen sulfide. Indeed, many of the biological actions of these gases can be accounted for by their ability to modulate ion channel activity. Here, we report recent evidence that H2 S is a modulator of low voltage-activated T-type Ca(2+) channels, and discriminates between the different subtypes of T-type Ca(2+) channel in that it selectively modulates Cav3.2, whilst Cav3.1 and Cav3.3 are unaffected. At high concentrations, H2 S augments Cav3.2 currents, an observation which has led to the suggestion that H2 S exerts its pro-nociceptive effects via this channel, since Cav3.2 plays a central role in sensory nerve excitability. However, at more physiological concentrations, H2 S is seen to inhibit Cav3.2. This inhibitory action requires the presence of the redox-sensitive, extracellular region of the channel which is responsible for tonic metal ion binding and which particularly distinguishes this channel isoform from Cav3.1 and 3.3. Further studies indicate that H2 S may act in a novel manner to alter channel activity by potentiating the zinc sensitivity/affinity of this binding site. This review discusses the different reports of H2 S modulation of T-type Ca(2+) channels, and how such varying effects may impact on nociception given the role of this channel in sensory activity. This subject remains controversial, and future studies are required before the impact of T-type Ca(2+) channel modulation by H2 S might be exploited as a novel approach to pain management.
离子通道代表了一个庞大且不断增长的靶蛋白家族,它们受一氧化氮、一氧化碳等气体递质调节,最近还发现受硫化氢调节。事实上,这些气体的许多生物学作用都可以通过它们调节离子通道活性的能力来解释。在此,我们报告最新证据表明,硫化氢是低电压激活的T型Ca(2+)通道的调节剂,并且它能区分T型Ca(2+)通道的不同亚型,因为它选择性地调节Cav3.2,而Cav3.1和Cav3.3不受影响。在高浓度时,硫化氢会增强Cav3.2电流,这一观察结果提示硫化氢可能通过该通道发挥其促痛觉过敏作用,因为Cav3.2在感觉神经兴奋性中起核心作用。然而,在更接近生理浓度时,硫化氢会抑制Cav3.2。这种抑制作用需要通道的氧化还原敏感的细胞外区域的存在,该区域负责静息金属离子结合,并且特别将该通道亚型与Cav3.1和3.3区分开来。进一步的研究表明,硫化氢可能以一种新的方式通过增强该结合位点的锌敏感性/亲和力来改变通道活性。本综述讨论了硫化氢对T型Ca(2+)通道调节的不同报道,以及鉴于该通道在感觉活动中的作用,这种不同的效应可能如何影响痛觉感受。这个问题仍然存在争议,在硫化氢对T型Ca(2+)通道的调节作用可能被用作一种新的疼痛管理方法之前,还需要进一步的研究。