Departamento de Farmacología, Facultad de Medicina, Universidad Nacional Autónoma de México, Ciudad de México 04510, México.
Departamento de Investigación en Hiperreactividad Bronquial, Instituto Nacional de Enfermedades Respiratorias, Ciudad de México 14080, México.
Int J Mol Med. 2018 Dec;42(6):2998-3008. doi: 10.3892/ijmm.2018.3910. Epub 2018 Oct 2.
In airway smooth muscle, the intracellular basal Ca2+ concentration [b(Ca2+)i] must be tightly regulated by several mechanisms in order to maintain a proper airway patency. The b[Ca2+]i is efficiently regulated by sarcoplasmic reticulum Ca2+‑ATPase 2b, plasma membrane Ca2+‑ATPase 1 or 4 and by the Na+/Ca2+ exchanger. Membranal Ca2+ channels, including the L‑type voltage dependent Ca2+ channel (L‑VDCC), T‑type voltage dependent Ca2+ channel (T‑VDCC) and transient receptor potential canonical 3 (TRPC3), appear to be constitutively active under basal conditions via the action of different signaling pathways, and are responsible for Ca2+ influx to maintain b[Ca2+]i. The two types of voltage‑dependent Ca2+ channels (L‑ and T‑type) are modulated by phosphorylation processes mediated by mitogen‑activated protein kinase kinase (MEK) and extracellular‑signal‑regulated kinase 1 and 2 (ERK1/2). The MEK/ERK signaling pathway can be activated by G‑protein‑coupled receptors through the αq subunit when the endogenous ligand (i.e., acetylcholine, histamine, leukotrienes, etc.) is present under basal conditions. It may also be stimulated when receptor tyrosine kinases are occupied by the appropriate ligand (cytokines, growth factors, etc.). ERK1/2 phosphorylates L‑VDCC on Ser496 of the β2 subunit and Ser1928 of the α1 subunit, decreasing or increasing the channel activity, respectively, and enabling it to switch between an open and closed state. T‑VDCC is also probably phosphorylated by ERK1/2, although further research is required to identify the phosphorylation sites. TRPC3 is directly activated by diacylglycerol produced by phospholipase C (PLCβ or γ). Constitutive inositol 1,4,5‑trisphosphate production induces the release of Ca2+ from the sarcoplasmic reticulum through inositol triphosphate receptor 1. This ion induces Ca2+‑induced Ca2+ release through the ryanodine receptor 2 (designated as Ca2+ 'sparks'). Therefore, several Ca2+ handling mechanisms are finely tuned to regulate basal intracellular Ca2+ concentrations. It is conceivable that alterations in any of these processes may render airway smooth muscle susceptible to develop hyperresponsiveness that is observed in ailments such as asthma.
在气道平滑肌中,细胞内基础钙离子浓度 [b(Ca2+)i] 必须通过几种机制来严格调节,以维持适当的气道通畅。b[Ca2+]i 由肌浆网 Ca2+-ATP 酶 2b、质膜 Ca2+-ATP 酶 1 或 4 和 Na+/Ca2+ 交换器有效调节。质膜 Ca2+ 通道,包括 L-型电压依赖性 Ca2+ 通道(L-VDCC)、T-型电压依赖性 Ca2+ 通道(T-VDCC)和瞬时受体电位经典型 3(TRPC3),在基础条件下似乎通过不同的信号通路持续激活,负责 Ca2+ 内流以维持 b[Ca2+]i。两种类型的电压依赖性 Ca2+ 通道(L- 和 T-型)通过丝裂原活化蛋白激酶激酶(MEK)和细胞外信号调节激酶 1 和 2(ERK1/2)介导的磷酸化过程调节。MEK/ERK 信号通路可被 G 蛋白偶联受体激活,当内源性配体(即乙酰胆碱、组胺、白三烯等)存在于基础条件下时,通过 αq 亚基。当适当的配体(细胞因子、生长因子等)占据受体酪氨酸激酶时,它也可能受到刺激。ERK1/2 在 L-VDCC 的 β2 亚基的 Ser496 和 α1 亚基的 Ser1928 上磷酸化 L-VDCC,分别降低或增加通道活性,使其在开放和关闭状态之间切换。TRPC3 也可能被 ERK1/2 磷酸化,尽管需要进一步研究来确定磷酸化位点。二酰基甘油由磷脂酶 C(PLCβ 或 γ)产生,直接激活 TRPC3。组成性肌醇 1,4,5-三磷酸的产生通过肌醇三磷酸受体 1 诱导肌浆网中 Ca2+ 的释放。这种离子通过肌浆网钙释放通道 2(称为 Ca2+“火花”)诱导 Ca2+-诱导的 Ca2+ 释放。因此,几种 Ca2+ 处理机制被精细调节以调节基础细胞内 Ca2+ 浓度。可以想象,这些过程中的任何改变都可能使气道平滑肌容易发展为哮喘等疾病中观察到的高反应性。