Department of Physiology and Biomedical Engineering, Mayo Clinic, Rochester, Minnesota, USA.
Division of Pulmonary and Critical Care Medicine, Department of Medicine, Brigham and Women's Hospital, Boston, Massachusetts, USA.
Physiol Rep. 2024 Apr;12(7):e15999. doi: 10.14814/phy2.15999.
Pulmonary arterial hypertension (PAH) causes pulmonary vascular remodeling, increasing pulmonary vascular resistance (PVR) and leading to right heart failure and death. Matrix stiffening early in the disease promotes remodeling in pulmonary artery smooth muscle cells (PASMCs), contributing to PAH pathogenesis. Our research identified YAP and TAZ as key drivers of the mechanobiological feedback loop in PASMCs, suggesting targeting them could mitigate remodeling. However, YAP/TAZ are ubiquitously expressed and carry out diverse functions, necessitating a cell-specific approach. Our previous work demonstrated that targeting non-canonical IKB kinase TBK1 reduced YAP/TAZ activation in human lung fibroblasts. Here, we investigate non-canonical IKB kinases TBK1 and IKKε in pulmonary hypertension (PH) and their potential to modulate PASMC pathogenic remodeling by regulating YAP/TAZ. We show that TBK1 and IKKε are activated in PASMCs in a rat PH model. Inflammatory cytokines, elevated in PAH, activate these kinases in human PASMCs. Inhibiting TBK1/IKKε expression/activity significantly reduces PAH-associated PASMC remodeling, with longer-lasting effects on YAP/TAZ than treprostinil, an approved PAH therapy. These results show that non-canonical IKB kinases regulate YAP/TAZ in PASMCs and may offer a novel approach for reducing vascular remodeling in PAH.
肺动脉高压 (PAH) 导致肺血管重构,增加肺血管阻力 (PVR),导致右心衰竭和死亡。疾病早期的基质变硬促进肺动脉平滑肌细胞 (PASMC) 的重塑,导致 PAH 的发病机制。我们的研究确定了 YAP 和 TAZ 是 PASMC 中机械生物学反馈环的关键驱动因素,表明靶向它们可能减轻重塑。然而,YAP/TAZ 广泛表达并发挥多种功能,需要一种细胞特异性的方法。我们之前的工作表明,靶向非典型 IKB 激酶 TBK1 可减少人肺成纤维细胞中 YAP/TAZ 的激活。在这里,我们研究了非典型 IKB 激酶 TBK1 和 IKKε 在肺动脉高压 (PH) 中的作用及其通过调节 YAP/TAZ 来调节 PASMC 致病重塑的潜力。我们表明,TBK1 和 IKKε 在大鼠 PH 模型中的 PASMC 中被激活。在 PAH 中升高的炎症细胞因子激活了这些激酶在人 PASMCs 中的活性。抑制 TBK1/IKKε 的表达/活性可显著减少与 PAH 相关的 PASMC 重塑,其对 YAP/TAZ 的作用比批准的 PAH 治疗药物曲前列尼尔更持久。这些结果表明,非典型 IKB 激酶调节 PASMC 中的 YAP/TAZ,并可能为减少 PAH 中的血管重塑提供一种新方法。