Vascular Biology Program, Department of Surgery, Boston Children's Hospital, Harvard Medical School, 11.211 Karp Family Research Bldg., 300 Longwood Ave., Boston, MA, 02115, USA.
Department of Chemistry and Biochemistry, Brigham Young University, Provo, UT, 84602, USA.
Angiogenesis. 2022 Aug;25(3):397-410. doi: 10.1007/s10456-022-09833-w. Epub 2022 Feb 25.
Anthrax protective antigen (PA) is a potent inhibitor of pathological angiogenesis with an unknown mechanism. In anthrax intoxication, PA interacts with capillary morphogenesis gene 2 (CMG2) and tumor endothelial marker 8 (TEM8). Here, we show that CMG2 mediates the antiangiogenic effects of PA and is required for growth-factor-induced chemotaxis. Using specific inhibitors of CMG2 and TEM8 interaction with natural ligand, as well as mice with the CMG2 or TEM8 transmembrane and intracellular domains disrupted, we demonstrate that inhibiting CMG2, but not TEM8 reduces growth-factor-induced angiogenesis in the cornea. Furthermore, the antiangiogenic effect of PA was abolished when the CMG2, but not the TEM8, gene was disrupted. Binding experiments demonstrated a broad ligand specificity for CMG2 among extracellular matrix (ECM) proteins. Ex vivo experiments demonstrated that CMG2 (but not TEM8) is required for PA activity in human dermal microvascular endothelial cell (HMVEC-d) network formation assays. Remarkably, blocking CMG2-ligand binding with PA or CRISPR knockout abolishes endothelial cell chemotaxis but not chemokinesis in microfluidic migration assays. These effects are phenocopied by Rho inhibition. Because CMG2 mediates the chemotactic response of endothelial cells to peptide growth factors in an ECM-dependent fashion, CMG2 is well-placed to integrate growth factor and ECM signals. Thus, CMG2 targeting is a novel way to inhibit angiogenesis.
炭疽保护性抗原(PA)是一种强效的病理性血管生成抑制剂,但作用机制未知。在炭疽中毒中,PA 与毛细血管形态发生基因 2(CMG2)和肿瘤内皮标志物 8(TEM8)相互作用。在这里,我们表明 CMG2 介导 PA 的抗血管生成作用,并且是生长因子诱导的趋化作用所必需的。使用 CMG2 与天然配体相互作用的特异性抑制剂以及 CMG2 或 TEM8 跨膜和细胞内结构域被破坏的小鼠,我们证明抑制 CMG2,但不是 TEM8,可减少角膜中的生长因子诱导的血管生成。此外,当破坏 CMG2 基因而不是 TEM8 基因时,PA 的抗血管生成作用被消除。结合实验证明了 CMG2 在细胞外基质(ECM)蛋白中具有广泛的配体特异性。离体实验表明,CMG2(而不是 TEM8)是 PA 活性在人真皮微血管内皮细胞(HMVEC-d)网络形成测定中的必需的。值得注意的是,用 PA 或 CRISPR 敲除阻断 CMG2-配体结合可抑制内皮细胞趋化性,但在微流体迁移测定中不抑制趋化运动。这些效应被 Rho 抑制所模拟。由于 CMG2 以 ECM 依赖性方式介导内皮细胞对肽生长因子的趋化反应,因此 CMG2 很好地整合了生长因子和 ECM 信号。因此,CMG2 靶向是抑制血管生成的一种新方法。