Department of Pharmaceutical Sciences, School of Pharmacy, North Dakota State University, Fargo, ND, USA.
Vanderbilt University Medical Center, Nashville, TN, USA.
Eur J Cell Biol. 2023 Jun;102(2):151316. doi: 10.1016/j.ejcb.2023.151316. Epub 2023 Apr 18.
The expression of the angiotensin-converting enzyme 2 (ACE2) is altered in multiple chronic kidney diseases like hypertension and renal fibrosis, where the signaling from the basal membrane proteins is critical for the development and progression of the various pathologies. Integrins are heterodimeric cell surface receptors that have important roles in the progression of these chronic kidney diseases by altering various cell signaling pathways in response to changes in the basement membrane proteins. It is unclear whether integrin or integrin-mediated signaling affects the ACE2 expression in the kidney. The current study tests the hypothesis that integrin β1 regulates the expression of ACE2 in kidney epithelial cells. The role of integrin β1 in ACE2 expression in renal epithelial cells was investigated by shRNA-mediated knockdown and pharmacological inhibition. In vivo studies were carried out using epithelial cell-specific deletion of integrin β1 in the kidneys. Deletion of integrin β1 from the mouse renal epithelial cells reduced the expression of ACE2 in the kidney. Furthermore, the downregulation of integrin β1 using shRNA decreased ACE2 expression in human renal epithelial cells. ACE2 expression levels were also decreased in renal epithelial cells and cancer cells when treated with an integrin α2β1 antagonist, BTT 3033. SARS-CoV-2 viral entry to human renal epithelial cells and cancer cells was also inhibited by BTT 3033. This study demonstrates that integrin β1 positively regulates the expression of ACE2, which is required for the entry of SARS-CoV-2 into kidney cells.
血管紧张素转换酶 2(ACE2)的表达在多种慢性肾脏疾病中发生改变,如高血压和肾纤维化,基底膜蛋白的信号对于各种病理的发展和进展至关重要。整合素是细胞表面的异二聚体受体,通过改变基底膜蛋白变化时的各种细胞信号通路,在这些慢性肾脏疾病的进展中发挥重要作用。目前尚不清楚整合素或整合素介导的信号是否会影响肾脏中 ACE2 的表达。本研究检验了以下假设:整合素β1 调节肾脏上皮细胞中 ACE2 的表达。通过 shRNA 介导的敲低和药理学抑制来研究整合素β1 在肾上皮细胞中 ACE2 表达中的作用。通过在肾脏中特异性敲除上皮细胞中的整合素β1 进行体内研究。从肾脏上皮细胞中敲除整合素β1 可降低肾脏中 ACE2 的表达。此外,shRNA 下调整合素β1 可降低人肾上皮细胞中 ACE2 的表达。当用整合素 α2β1 拮抗剂 BTT 3033 处理时,肾上皮细胞和癌细胞中的 ACE2 表达水平也降低。BTT 3033 抑制 SARS-CoV-2 病毒进入人肾上皮细胞和癌细胞。本研究表明,整合素β1 正向调节 ACE2 的表达,这是 SARS-CoV-2 进入肾细胞所必需的。