Cell Division and Cancer Group, Spanish National Cancer Research Centre (CNIO), Madrid, Spain.
Gene Regulation in Cardiovascular Remodelling and Inflammation Group, Spanish National Cardiovascular Centre (CNIC), Madrid, Spain.
Nat Med. 2017 Aug;23(8):964-974. doi: 10.1038/nm.4364. Epub 2017 Jul 10.
Polo-like kinase 1 (PLK1), an essential regulator of cell division, is currently undergoing clinical evaluation as a target for cancer therapy. We report an unexpected function of Plk1 in sustaining cardiovascular homeostasis. Plk1 haploinsufficiency in mice did not induce obvious cell proliferation defects but did result in arterial structural alterations, which frequently led to aortic rupture and death. Specific ablation of Plk1 in vascular smooth muscle cells (VSMCs) led to reduced arterial elasticity, hypotension, and an impaired arterial response to angiotensin II in vivo. Mechanistically, we found that Plk1 regulated angiotensin II-dependent activation of RhoA and actomyosin dynamics in VSMCs in a mitosis-independent manner. This regulation depended on Plk1 kinase activity, and the administration of small-molecule Plk1 inhibitors to angiotensin II-treated mice led to reduced arterial fitness and an elevated risk of aneurysm and aortic rupture. We thus conclude that a partial reduction of Plk1 activity that does not block cell division can nevertheless impair aortic homeostasis. Our findings have potentially important implications for current approaches aimed at PLK1 inhibition for cancer therapy.
丝氨酸/苏氨酸激酶 Polo 样激酶 1(PLK1)是细胞分裂的重要调节因子,目前正在进行临床试验,作为癌症治疗的靶点。我们报告了 Plk1 在维持心血管稳态中的一个意外功能。在小鼠中 Plk1 单倍不足不会引起明显的细胞增殖缺陷,但会导致动脉结构改变,这常常导致主动脉破裂和死亡。特异性消融血管平滑肌细胞(VSMCs)中的 Plk1 会导致动脉弹性降低、低血压和对血管紧张素 II 的动脉反应受损。在机制上,我们发现 Plk1 以有丝分裂独立的方式调节血管紧张素 II 依赖性 RhoA 和肌动球蛋白动力学的激活。这种调节依赖于 Plk1 激酶活性,并且向血管紧张素 II 处理的小鼠施用小分子 Plk1 抑制剂会导致动脉适应性降低和动脉瘤和主动脉破裂的风险增加。因此,我们得出结论,不会阻止细胞分裂的 Plk1 活性的部分降低仍会损害主动脉稳态。我们的发现可能对目前旨在抑制 PLK1 以治疗癌症的方法具有重要意义。