Doçi Colleen L, Mikelis Constantinos M, Callejas-Valera Juan Luis, Hansen Karina K, Molinolo Alfredo A, Inoue Asuka, Offermanns Stefan, Gutkind J Silvio
College of Arts and Sciences, Marian University Indianapolis, Indianapolis, Indiana, United States of America.
Department of Biomedical Sciences, School of Pharmacy, Texas Tech University Health Sciences Center, Amarillo, Texas, United States of America.
PLoS One. 2017 Mar 16;12(3):e0173692. doi: 10.1371/journal.pone.0173692. eCollection 2017.
G-protein coupled receptors (GPCRs), which activate heterotrimeric G proteins, are an essential class of transmembrane receptors that are responsible for a myriad of signaling events in normal and pathologic conditions. Two members of the G protein family, Gαq and Gα11, activate one of the main GPCR pathways and function as oncogenes by integrating mitogen-stimulated signaling cascades that are active under malignant conditions. Recently, it has been shown that targeted deletion of Gα11 and Gαq from endothelial cells impairs the Rho-mediated formation of focal adherens junctions, suggesting that Gα11/q signaling may also play a significant role in cytoskeletal-mediated cellular responses in epithelial cells. Indeed, combined deletion of Gα11 and Gαq confers a significant migratory defect in keratinocytes that delays cutaneous wound healing in an in vivo setting. This delay can be attributed to a defect during the reepithelialization phase due to significantly attenuated migratory capacity of Gαq-null keratinocytes under combined Gα11 deficiency. In fact, cells lacking Gα11/q demonstrate a severely reduced ability to respond to mitogenic and migratory signals in the microenvironment, leading to inappropriate and premature terminal differentiation. These results suggest that Gα11/q signaling pathways may be critical for integrating mitogenic signals and cytoskeletal function to achieve normal physiological responses. Emergence of a malignant phenotype may therefore arise from both under- and overexpression of Gα11/q signaling, implicating its upstream regulation as a potential therapeutic target in a host of pathologic conditions.
G蛋白偶联受体(GPCRs)可激活异源三聚体G蛋白,是一类重要的跨膜受体,在正常和病理条件下负责无数的信号转导事件。G蛋白家族的两个成员Gαq和Gα11激活主要的GPCR途径之一,并通过整合在恶性条件下活跃的有丝分裂原刺激信号级联反应而发挥癌基因的作用。最近的研究表明,内皮细胞中Gα11和Gαq的靶向缺失会损害Rho介导的粘着斑连接的形成,这表明Gα11/q信号传导在上皮细胞的细胞骨架介导的细胞反应中也可能起重要作用。事实上,Gα11和Gαq的联合缺失赋予角质形成细胞明显的迁移缺陷,在体内延迟皮肤伤口愈合。这种延迟可归因于再上皮化阶段的缺陷,这是由于在Gα11联合缺乏的情况下,Gαq缺失的角质形成细胞迁移能力显著减弱。实际上,缺乏Gα11/q的细胞对微环境中有丝分裂和迁移信号的反应能力严重降低,导致不适当和过早的终末分化。这些结果表明,Gα11/q信号通路对于整合有丝分裂信号和细胞骨架功能以实现正常生理反应可能至关重要。因此,恶性表型的出现可能源于Gα11/q信号传导的低表达和高表达,这意味着其上游调控作为许多病理条件下的潜在治疗靶点。