Department of Molecular and Cellular Pharmacology, University of Miami Miller School of Medicine, Miami, Florida, USA; Sylvester Comprehensive Cancer Center, University of Miami Miller School of Medicine, Miami, Florida, USA.
Department of Molecular and Cellular Pharmacology, University of Miami Miller School of Medicine, Miami, Florida, USA.
J Biol Chem. 2024 May;300(5):107257. doi: 10.1016/j.jbc.2024.107257. Epub 2024 Apr 2.
The Hippo signaling is instrumental in regulating organ size, regeneration, and carcinogenesis. The cytoskeleton emerges as a primary Hippo signaling modulator. Its structural alterations in response to environmental and intrinsic stimuli control Hippo signaling pathway activity. However, the precise mechanisms underlying the cytoskeleton regulation of Hippo signaling are not fully understood. RAP2 GTPase is known to mediate the mechanoresponses of Hippo signaling via activating the core Hippo kinases LATS1/2 through MAP4Ks and MST1/2. Here we show the pivotal role of the reciprocal regulation between RAP2 GTPase and the cytoskeleton in Hippo signaling. RAP2 deletion undermines the responses of the Hippo pathway to external cues tied to RhoA GTPase inhibition and actin cytoskeleton remodeling, such as energy stress and serum deprivation. Notably, RhoA inhibitors and actin disruptors fail to activate LATS1/2 effectively in RAP2-deficient cells. RNA sequencing highlighted differential regulation of both actin and microtubule networks by RAP2 gene deletion. Consistently, Taxol, a microtubule-stabilizing agent, was less effective in activating LATS1/2 and inhibiting cell growth in RAP2 and MAP4K4/6/7 knockout cells. In summary, our findings position RAP2 as a central integrator of cytoskeletal signals for Hippo signaling, which offers new avenues for understanding Hippo regulation and therapeutic interventions in Hippo-impaired cancers.
Hippo 信号通路在调节器官大小、再生和致癌作用中起着重要作用。细胞骨架作为 Hippo 信号的主要调节剂出现。它对环境和内在刺激的结构改变控制 Hippo 信号通路的活性。然而,细胞骨架调节 Hippo 信号的确切机制尚不完全清楚。RAP2 GTPase 已知通过激活核心 Hippo 激酶 LATS1/2 通过 MAP4Ks 和 MST1/2 来介导 Hippo 信号的机械反应。在这里,我们展示了 RAP2 GTPase 和细胞骨架在 Hippo 信号中的相互调节在 Hippo 信号中的关键作用。RAP2 的缺失破坏了 Hippo 途径对与 RhoA GTPase 抑制和肌动球蛋白细胞骨架重塑相关的外部线索的反应,例如能量应激和血清剥夺。值得注意的是,RhoA 抑制剂和肌动蛋白破坏剂在 RAP2 缺陷细胞中不能有效地激活 LATS1/2。RNA 测序突出了 RAP2 基因缺失对肌动蛋白和微管网络的差异调节。一致地,紫杉醇,一种微管稳定剂,在激活 LATS1/2 和抑制 RAP2 和 MAP4K4/6/7 敲除细胞中的细胞生长方面效果较差。总之,我们的发现将 RAP2 定位为 Hippo 信号细胞骨架信号的中央整合者,为理解 Hippo 调节和 Hippo 受损癌症的治疗干预提供了新的途径。